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ChEMBL ligand: CHEMBL57 (BIRG 0587, BIRG-0587, Nevirapina, Nevirapine, Nevirapine anhydrous, Nevirapine, anhydrous, Nevirapine teva, Nevirapinum anhydrous, NSC-641530, Viramune, Viramune xr) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
---|---|---|---|---|---|---|---|---|
Human immunodeficiency virus type 1 protease in Human immunodeficiency virus 1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL243] [UniProtKB: Q72874] | ||||||||
ChEMBL | Inhibition single mutant of HIV-1 RT (K103 N) | B | 4.24 | pIC50 | 57900 | nM | IC50 | J Med Chem (1993) 36: 1291-1294 [PMID:7683725] |
ChEMBL | Inhibition single mutant of HIV-1 RT (Y181C) | B | 4.95 | pIC50 | 11300 | nM | IC50 | J Med Chem (1993) 36: 1291-1294 [PMID:7683725] |
ChEMBL | Inhibition of HIV-1 RT using rC-dG as template | B | 7 | pIC50 | 101 | nM | IC50 | J Med Chem (1993) 36: 1291-1294 [PMID:7683725] |
Human immunodeficiency virus type 1 reverse transcriptase in Human immunodeficiency virus 1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL247] [UniProtKB: Q72547] | ||||||||
ChEMBL | Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 Y181I mutant expressed in Escherichia coli JM109 | B | 4.44 | pKi | 36000 | 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 | 4.44 | pKi | 36000 | nM | Ki | J Med Chem (2001) 44: 305-315 [PMID:11462972] |
ChEMBL | In vitro inhibitory activity against HIV-1 mutant Reverse transcriptase containing the single amino acid substitution Y181I | B | 4.44 | pKi | 36000 | nM | Ki | J Med Chem (1999) 42: 4462-4470 [PMID:10543890] |
ChEMBL | Inhibition of HIV1 reverse transcriptase Y188L mutant | B | 4.74 | pKi | 18000 | nM | Ki | J Med Chem (2007) 50: 5412-5424 [PMID:17910429] |
ChEMBL | In vitro inhibitory activity against HIV-1 mutant Reverse transcriptase containing the single amino acid substitution Y188L | B | 4.74 | pKi | 18000 | nM | Ki | J Med Chem (1999) 42: 4462-4470 [PMID:10543890] |
ChEMBL | Inhibition of HIV-1 Mutant HIV-1 RT enzymes containing the single amino acid substitution Y188L | B | 4.74 | pKi | 18000 | nM | Ki | J Med Chem (2001) 44: 305-315 [PMID:11462972] |
ChEMBL | Inhibition of HIV1 reverse transcriptase V106A mutant | B | 5 | pKi | 10000 | nM | Ki | J Med Chem (2007) 50: 5412-5424 [PMID:17910429] |
ChEMBL | Inhibition of HIV-1 Mutant HIV-1 RT enzymes containing the single amino acid substitution V106A | B | 5 | pKi | 10000 | nM | Ki | J Med Chem (2001) 44: 305-315 [PMID:11462972] |
ChEMBL | In vitro inhibitory activity against HIV-1 mutant Reverse transcriptase containing the single amino acid substitution V106A | B | 5 | pKi | 10000 | nM | Ki | J Med Chem (1999) 42: 4462-4470 [PMID:10543890] |
ChEMBL | Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 L100I mutant expressed in Escherichia coli JM109 | B | 5.05 | pKi | 9000 | 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 | 5.05 | pKi | 9000 | nM | Ki | J Med Chem (2001) 44: 305-315 [PMID:11462972] |
ChEMBL | Inhibition of HIV1 reverse transcriptase L100I mutant | B | 5.05 | pKi | 9000 | nM | Ki | J Med Chem (2007) 50: 5412-5424 [PMID:17910429] |
ChEMBL | In vitro inhibitory activity against HIV-1 mutant Reverse transcriptase containing the single amino acid substitution L100I | B | 5.05 | pKi | 9000 | nM | Ki | J Med Chem (1999) 42: 4462-4470 [PMID:10543890] |
ChEMBL | Non-competitive inhibition of wild type HIV1 reverse transcriptase p66/p51 after 30 mins by liquid scintillation counting | B | 5.14 | pKi | 7200 | nM | Ki | Bioorg Med Chem (2013) 21: 1150-1158 [PMID:23357038] |
ChEMBL | Inhibition of HIV1 reverse transcriptase K103N mutant | B | 5.15 | pKi | 7000 | nM | Ki | J Med Chem (2007) 50: 5412-5424 [PMID:17910429] |
ChEMBL | In vitro inhibitory activity against HIV-1 mutant Reverse transcriptase containing the single amino acid substitution K103N | B | 5.15 | pKi | 7000 | nM | Ki | J Med Chem (1999) 42: 4462-4470 [PMID:10543890] |
ChEMBL | Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 K103N mutant expressed in Escherichia coli JM109 | B | 5.15 | pKi | 7000 | 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 K103N | B | 5.15 | pKi | 7000 | 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 | 5.3 | pKi | 5000 | 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 | 5.4 | pKi | 4000 | nM | Ki | J Med Chem (2009) 52: 840-851 [PMID:19140683] |
ChEMBL | Inhibition of HIV1 recombinant reverse transcriptase K103N mutant-DNA binary complex expressed in Escherichia coli BL21 | B | 5.4 | pKi | 4000 | nM | Ki | J Med Chem (2009) 52: 840-851 [PMID:19140683] |
ChEMBL | Inhibition of wild type HIV1 reverse transcriptase-DNA binary complex | B | 6.3 | pKi | 500 | nM | Ki | J Med Chem (2009) 52: 840-851 [PMID:19140683] |
ChEMBL | Inhibition of HIV-1 wild-type RT | B | 6.4 | pKi | 400 | 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 expressed in Escherichia coli JM109 | B | 6.4 | pKi | 400 | nM | Ki | J Med Chem (2009) 52: 1224-1228 [PMID:19170521] |
ChEMBL | Inhibition of wild type HIV1 reverse transcriptase-DNA-dNTP ternary complex | B | 6.4 | pKi | 400 | nM | Ki | J Med Chem (2009) 52: 840-851 [PMID:19140683] |
ChEMBL | Inhibition of wild type HIV1 free reverse transcriptase | B | 6.4 | pKi | 400 | nM | Ki | J Med Chem (2009) 52: 840-851 [PMID:19140683] |
ChEMBL | Inhibition of wild type HIV1 3B reverse transcriptase | B | 6.4 | pKi | 400 | nM | Ki | J Med Chem (2007) 50: 5412-5424 [PMID:17910429] |
ChEMBL | In vitro inhibitory activity against HIV-1 wild type reverse transcriptase (RT) | B | 6.4 | pKi | 400 | nM | Ki | J Med Chem (1999) 42: 4462-4470 [PMID:10543890] |
ChEMBL | Inhibition of HIV1 reverse transcriptase V179D mutant | B | 6.52 | pKi | 300 | nM | Ki | J Med Chem (2007) 50: 5412-5424 [PMID:17910429] |
ChEMBL | Inhibitory activity against non-nucleoside reverse transcriptase inhibitors (NNRTI) -resistant HIV-1 strain A17 with a Y181C mutation in RT (reverse transcriptase) | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 523-528 [PMID:11229762] |
ChEMBL | Inhibition of DNA dependent DNA polymerase activity of HIV1 reverse transcriptase Y181C mutant expressed in Escherichia coli BL21 | B | 4 | pIC50 | 100000 | nM | IC50 | J Med Chem (2008) 51: 5702-5713 [PMID:18800765] |
ChEMBL | Inhibitory activity against non-nucleoside reverse transcriptase inhibitors (NNRTI) -resistant HIV-1 strain A17 variant with Y181C plus K103N mutations in RT (reverse transcriptase) | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 523-528 [PMID:11229762] |
ChEMBL | Concentration required for 50% inhibition of human immunodeficiency virus type 1 reverse transcriptase Ile100 | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2004) 47: 5912-5922 [PMID:15537346] |
ChEMBL | Fold increase in inhibitory concentration against HIV 1 reverse transcriptase mutant type Ile100 over wild type HIV 1 reverse transcriptase | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2004) 47: 5912-5922 [PMID:15537346] |
ChEMBL | Concentration required for 50% inhibition of human immunodeficiency virus type 1 reverse transcriptase mutant type Cys181 | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2004) 47: 5912-5922 [PMID:15537346] |
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 | 4.17 | pIC50 | 67600 | nM | IC50 | Eur J Med Chem (2021) 226: 113868-113868 [PMID:34583311] |
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 | 4.17 | pIC50 | >67000 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 4667-4672 [PMID:19704127] |
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 | 4.17 | pIC50 | >67000 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 4667-4672 [PMID:19704127] |
ChEMBL | In vitro inhibition of mutant Y181C recombinant reverse transcriptase of HIV-1 IIIB | B | 4.22 | pIC50 | >60000 | nM | IC50 | J Med Chem (1996) 39: 3769-3789 [PMID:8809165] |
ChEMBL | Inhibition of HIV1 RT Y181I mutant | B | 4.44 | pIC50 | 36000 | nM | IC50 | J Med Chem (2005) 48: 7153-7165 [PMID:16279773] |
ChEMBL | Inhibition of wild type HIV-1 reverse transcriptase using biotin-labelled dNTPs as substrate incubated for 2 hrs by ELISA | B | 4.51 | pIC50 | 31000 | nM | IC50 | J Med Chem (2022) 65: 2458-2470 [PMID:35061384] |
ChEMBL | Inhibition of HIV1 reverse transcriptase Y181I mutant by RNA-dependent DNA polymerase activity assay | B | 4.52 | pIC50 | 30000 | nM | IC50 | Bioorg Med Chem (2010) 18: 1702-1710 [PMID:20097079] |
ChEMBL | Inhibition of HIV1 reverse transcriptase using Poly rA.dT template | B | 4.64 | pIC50 | 23000 | nM | IC50 | Eur J Med Chem (2007) 42: 993-1003 [PMID:17321639] |
ChEMBL | Inhibitory activity against recombinant HIV-1 reverse transcriptase (rRT) | B | 4.64 | pIC50 | 23000 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 2721-2726 [PMID:10509923] |
ChEMBL | Inhibition of recombinant reverse transcriptase (RT) in cell-free Quan-T-RT assay system | B | 4.64 | pIC50 | 23000 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 3411-3416 [PMID:10617082] |
ChEMBL | Compound was evaluated for its inhibitory activity against recombinant HIV-1 Reverse transcriptase using cell free RT inhibition assay | B | 4.64 | pIC50 | 23000 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2071-2074 [PMID:10999473] |
ChEMBL | Inhibition of purified recombinant HIV-1 reverse transcriptase | B | 4.64 | pIC50 | 23000 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1593-1598 [PMID:10386942] |
ChEMBL | Inhibition of wild type HIV1 reverse transcriptase Y181I 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 Y181I/Y181C 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 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 | 4.7 | pIC50 | >20000 | 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 | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (2014) 57: 9945-9957 [PMID:25418038] |
ChEMBL | Inhibitory activity against HIV rRT activity in mutant HIV-1 strain resistant to Nevirapine (Y181C) | B | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (1996) 39: 522-530 [PMID:8558522] |
ChEMBL | Inhibition of HIV1 RT Y188L mutant | B | 4.74 | pIC50 | 18000 | nM | IC50 | J Med Chem (2005) 48: 7153-7165 [PMID:16279773] |
ChEMBL | Inhibition of HIV1 reverse transcriptase p66/p51 L100I mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry | B | 4.85 | pIC50 | 14000 | nM | IC50 | Bioorg Med Chem (2016) 24: 2476-2485 [PMID:27112451] |
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 | 4.85 | pIC50 | 14000 | nM | IC50 | Bioorg Med Chem (2017) 25: 3861-3870 [PMID:28559060] |
ChEMBL | Inhibition of HIV1 reverse transcriptase after 1 hr by ELISA | B | 4.88 | pIC50 | 13200 | nM | IC50 | Eur J Med Chem (2010) 45: 4096-4103 [PMID:20598780] |
ChEMBL | Inhibitory effect on recombinant HIV- 1 reverse transcriptase which has a mutation Leu 100 to Ile 100 (clone 118) | B | 4.89 | pIC50 | 13000 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 1511-1516 [PMID:9873380] |
ChEMBL | Inhibition of reverse transcriptase activity in HIV1 NL4-3 infected MT4 cells after dialysis | B | 4.92 | pIC50 | 12000 | nM | IC50 | Antimicrob Agents Chemother (2007) 51: 638-644 [PMID:17116672] |
ChEMBL | Tested for the inhibition of mutant type (Ile100) HIV-1 (IIIB) RT | B | 4.93 | pIC50 | 11800 | nM | IC50 | J Med Chem (1996) 39: 4261-4274 [PMID:8863804] |
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 | 4.96 | pIC50 | 11000 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 4667-4672 [PMID:19704127] |
ChEMBL | Inhibition of HIV1 reverse transcriptase by ELISA | B | 4.97 | pIC50 | 10600 | nM | IC50 | Bioorg Med Chem (2007) 15: 7399-7407 [PMID:17870545] |
ChEMBL | Inhibition of HIV1 RT V106A mutant | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2005) 48: 7153-7165 [PMID:16279773] |
ChEMBL | Inhibition of HIV1 isolate R8 reverse transcriptase K103N mutant after 90 mins by electrochemiluminescence analysis | B | 5.03 | pIC50 | 9300 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 2424-2431 [PMID:19289522] |
ChEMBL | Inhibition of HIV1 reverse transcriptase L100I mutant | B | 5.05 | pIC50 | 9000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3935-3938 [PMID:21636271] |
ChEMBL | Inhibition of HIV1 reverse transcriptase L100I mutant RNA-dependent DNA polymerase activity using poly(rA)/oligo(dT)10:1 and [3H]-dTTP substrate | B | 5.05 | pIC50 | 9000 | nM | IC50 | J Med Chem (2012) 55: 6634-6638 [PMID:22712652] |
ChEMBL | Inhibition of HIV1 RT L100I mutant | B | 5.05 | pIC50 | 9000 | nM | IC50 | J Med Chem (2005) 48: 7153-7165 [PMID:16279773] |
ChEMBL | Inhibition of wild type HIV1 reverse transcriptase L100I mutant assessed as reduction in enzyme activity | B | 5.05 | pIC50 | 9000 | nM | IC50 | J Med Chem (2014) 57: 9945-9957 [PMID:25418038] |
ChEMBL | Inhibition of HIV1 wild-type reverse transcriptase L100I mutant using [3H]dTTP by scintillation counting | B | 5.05 | pIC50 | 9000 | nM | IC50 | Eur J Med Chem (2014) 80: 101-111 [PMID:24769348] |
ChEMBL | Inhibition of HIV1 isolate R8 reverse transcriptase Y181C mutant after 90 mins by electrochemiluminescence analysis | B | 5.05 | pIC50 | 8900 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 2424-2431 [PMID:19289522] |
ChEMBL | Inhibition of wild type HIV1 Reverse transcriptase assessed as reduction of biotin deoxyuridine triphosphate incorporation into the wild type HIV1 reverse transcriptase after 1 hr by ELISA | B | 5.06 | pIC50 | 8800 | nM | IC50 | Eur J Med Chem (2016) 115: 53-62 [PMID:26994843] |
ChEMBL | Inhibition of HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation using poly(rA)-oligo(dT) as template/primer and digoxigenin-dUTP/biotin-dUTP/dTTP nucleotides incubated for 1 hr by ELISA | B | 5.06 | pIC50 | 8800 | nM | IC50 | Eur J Med Chem (2016) 109: 294-304 [PMID:26802545] |
ChEMBL | Inhibition of HIV-1 reverse transcriptase assessed as reduction in biotin-duTP incorporation using biotin-labeled dUTP and hybrid poly(A)-oligo (dT)15 template primer after 2 hrs by ELISA | B | 5.06 | pIC50 | 8780 | nM | IC50 | Bioorg Med Chem (2016) 24: 4424-4433 [PMID:27501911] |
ChEMBL | Inhibition of HIV-1 reverse transcriptase assessed as decrease in incorporation of [3H]TTP into polyA template | B | 5.12 | pIC50 | 7500 | nM | IC50 | J Nat Prod (2013) 76: 530-537 [PMID:23550966] |
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 | 5.14 | pIC50 | 7200 | 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 | 5.14 | pIC50 | 7200 | nM | IC50 | Medchemcomm (2013) 4: 1443-1451 |
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 | 5.15 | pIC50 | 7130 | nM | IC50 | Eur J Med Chem (2021) 226: 113868-113868 [PMID:34583311] |
ChEMBL | Inhibition of HIV1 reverse transcriptase K103N mutant | B | 5.15 | pIC50 | 7000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3935-3938 [PMID:21636271] |
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 | 5.15 | pIC50 | 7000 | nM | IC50 | J Med Chem (2012) 55: 6634-6638 [PMID:22712652] |
ChEMBL | Inhibition of HIV1 wild-type reverse transcriptase K103N mutant using [3H]dTTP by scintillation counting | B | 5.15 | pIC50 | 7000 | nM | IC50 | Eur J Med Chem (2014) 80: 101-111 [PMID:24769348] |
ChEMBL | Inhibition of RNA-dependent DNA polymerase activity of recombinant HIV-1 p66/p51 reverse transcriptase K103N mutant assessed as inhibition of [3H]dTTP incorporation using poly(rA)/oligo(dT) as templates incubated for 15 mins by MicroBeta scintillation counting method | B | 5.15 | pIC50 | 7000 | nM | IC50 | Eur J Med Chem (2020) 208: 112696-112696 [PMID:32883642] |
ChEMBL | Inhibition of HIV1 RT K103N mutant | B | 5.15 | pIC50 | 7000 | nM | IC50 | J Med Chem (2005) 48: 7153-7165 [PMID:16279773] |
ChEMBL | Inhibition of wild type HIV1 reverse transcriptase K103N mutant assessed as reduction in enzyme activity | B | 5.15 | pIC50 | 7000 | nM | IC50 | J Med Chem (2014) 57: 9945-9957 [PMID:25418038] |
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 | 5.15 | pIC50 | 7000 | nM | IC50 | J Med Chem (2017) 60: 6528-6547 [PMID:28628334] |
ChEMBL | Inhibition of HIV1 reverse transcriptase L100I mutant by RNA-dependent DNA polymerase activity assay | B | 5.15 | pIC50 | 7000 | nM | IC50 | Bioorg Med Chem (2010) 18: 1702-1710 [PMID:20097079] |
ChEMBL | Inhibition of HIV1 reverse transcriptase Y181C mutant in 293T cells | B | 5.18 | pIC50 | 6650 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 3034-3038 [PMID:16527484] |
ChEMBL | Inhibitory activity against HIV-1 reverse transcriptase | B | 5.19 | pIC50 | 6440 | nM | IC50 | J Med Chem (1996) 39: 1645-1650 [PMID:8648604] |
ChEMBL | Ability to inhibit HIV-1 IIIB reverse transcriptase catalyzed incorporation of tritiated thymidine triphosphate onto a biotinylated rA.dT template primer | B | 5.19 | pIC50 | 6440 | nM | IC50 | Bioorg Med Chem Lett (1992) 2: 1745-1750 |
ChEMBL | Inhibition of HIV1 reverse transcriptase assessed as inhibition of biotinylated dUTP incorporation after 1 hr by ELISA | B | 5.21 | pIC50 | 6200 | nM | IC50 | Bioorg Med Chem (2013) 21: 7091-7100 [PMID:24119448] |
ChEMBL | Activity of selected HIV-1 N-acylthiocarbamates in enzyme assay against Virion-Associated reverse transcriptase | B | 5.22 | pIC50 | 6000 | nM | IC50 | J Med Chem (2003) 46: 768-781 [PMID:12593657] |
ChEMBL | Inhibition of HIV1 reverse transcriptase K103N mutant in 293T cells | B | 5.24 | pIC50 | 5750 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 3034-3038 [PMID:16527484] |
ChEMBL | In vitro inhibition of HIV-1 reverse transcriptase | B | 5.26 | pIC50 | 5500 | nM | IC50 | J Med Chem (1993) 36: 1505-1508 [PMID:7684450] |
ChEMBL | Inhibition of HIV1 RT K103N mutant mediated DNA-dependent DNA polymerization using RNA PPT primed substrate by scintillation proximity assay | B | 5.3 | pIC50 | >5000 | nM | IC50 | J Biol Chem (2007) 282: 8005-8010 [PMID:17172472] |
ChEMBL | Inhibition of HIV1 RT K103N mutant mediated DNA-dependent DNA polymerization using DNA PPT primed substrate by scintillation proximity assay | B | 5.3 | pIC50 | >5000 | nM | IC50 | J Biol Chem (2007) 282: 8005-8010 [PMID:17172472] |
ChEMBL | Inhibition of HIV1 RT Y181C mutant mediated DNA-dependent DNA polymerization using RNA/DNAM duplex primed substrate by scintillation proximity assay | B | 5.3 | pIC50 | >5000 | nM | IC50 | J Biol Chem (2007) 282: 8005-8010 [PMID:17172472] |
ChEMBL | Inhibition of HIV1 RT Y181C mutant mediated DNA-dependent DNA polymerization using RNA PPT primed substrate by scintillation proximity assay | B | 5.3 | pIC50 | >5000 | nM | IC50 | J Biol Chem (2007) 282: 8005-8010 [PMID:17172472] |
ChEMBL | Inhibition of HIV1 RT Y181C mutant mediated DNA-dependent DNA polymerization using DNA PPT primed substrate by scintillation proximity assay | B | 5.3 | pIC50 | >5000 | nM | IC50 | J Biol Chem (2007) 282: 8005-8010 [PMID:17172472] |
ChEMBL | Inhibition of HIV1 RT K103N mutant mediated DNA-dependent DNA polymerization using RNA/DNAM duplex primed substrate by scintillation proximity assay | B | 5.3 | pIC50 | >5000 | nM | IC50 | J Biol Chem (2007) 282: 8005-8010 [PMID:17172472] |
ChEMBL | The compound was evaluated for the inhibition of HIV-1 reverse transcriptase | B | 5.31 | pIC50 | 4848 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 193-195 [PMID:10673109] |
ChEMBL | Inhibition of HIV-1 reverse transcriptase. | B | 5.31 | pIC50 | 4848 | nM | IC50 | J Med Chem (2000) 43: 2019-2030 [PMID:10821714] |
ChEMBL | Inhibition of HIV-1 recombinant reverse transcriptase after 1 hr by streptavidinalkaline phosphatase reporter system | B | 5.33 | pIC50 | 4650 | nM | IC50 | Bioorg Med Chem (2015) 23: 149-159 [PMID:25468035] |
ChEMBL | Inhibition of HIV1 reverse transcriptase after 1 hr by colorimetric assay | B | 5.35 | pIC50 | 4450 | nM | IC50 | J Med Chem (2013) 56: 3593-3608 [PMID:23540737] |
ChEMBL | Inhibition of HIV1 wild type RT using poly(rA)/oligo(dT)15 homopolymer template after 1 hrs by ELISA | B | 5.36 | pIC50 | 4400 | nM | IC50 | Bioorg Med Chem (2011) 19: 4366-4376 [PMID:21683601] |
ChEMBL | Inhibition of HIV-1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation into enzyme by colorimetry | B | 5.36 | pIC50 | 4390 | nM | IC50 | Eur J Med Chem (2011) 46: 5039-5045 [PMID:21872971] |
ChEMBL | Inhibition of HIV1 reverse transcriptase using poly(ra)/oligo(dT)15 homopolymer template as substrate after 1 hr | B | 5.39 | pIC50 | 4120 | nM | IC50 | J Med Chem (2012) 55: 2242-2250 [PMID:22283377] |
ChEMBL | Inhibition of biotin-dUTP labeled HIV-1 reverse transcriptase after 30 mins colorimetric streptavidin alkaline phosphatase reporter system | B | 5.39 | pIC50 | 4120 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3003-3005 [PMID:20347295] |
ChEMBL | Inhibition of HIV1 reverse transcriptase by ELISA | B | 5.39 | pIC50 | 4120 | nM | IC50 | Bioorg Med Chem (2010) 18: 3231-3237 [PMID:20371182] |
ChEMBL | Inhibition of RNA-dependent DNA polymerase activity of wild type HIV1 subtype B reverse transcriptase by filter-based filtration assay | B | 5.39 | pIC50 | 4100 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 2401-2408 [PMID:20308384] |
ChEMBL | Inhibition of HIV1 reverse transcriptase K103N mutant by RNA-dependent DNA polymerase activity assay | B | 5.4 | pIC50 | 4000 | nM | IC50 | Bioorg Med Chem (2010) 18: 1702-1710 [PMID:20097079] |
ChEMBL | Inhibitory activity against HIV-1 Mutant Reverse transcriptase V106A | B | 5.41 | pIC50 | 3930 | nM | IC50 | J Med Chem (1998) 41: 2972-2984 [PMID:9685236] |
ChEMBL | Inhibitory activity against HIV rRT activity in HIV-1 mutant resistant to TIBO(L100I) strain | B | 5.46 | pIC50 | 3500 | nM | IC50 | J Med Chem (1996) 39: 522-530 [PMID:8558522] |
ChEMBL | Compound was tested for inhibitory activity against HIV-1 mutant type reverse transcriptase (Y181C) | B | 5.49 | pIC50 | 3200 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 2169-2172 [PMID:9873507] |
ChEMBL | Inhibition of DNA-dependent DNA polymerase activity of wild type HIV1 subtype B reverse transcriptase by gel-based primer extension assay | B | 5.49 | pIC50 | 3200 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 2401-2408 [PMID:20308384] |
ChEMBL | In vitro ability to inhibit wild type resistant (WT) reverse transcriptase | B | 5.51 | pIC50 | 3100 | nM | IC50 | J Med Chem (2000) 43: 1034-1040 [PMID:10715167] |
ChEMBL | In vitro inhibition of recombinant reverse transcriptase (WT) of HIV-1 IIIB | B | 5.51 | pIC50 | 3100 | nM | IC50 | J Med Chem (1996) 39: 3769-3789 [PMID:8809165] |
ChEMBL | Inhibitory concentration against HIV-Reverse transcriptase | B | 5.52 | pIC50 | 3000 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1107-1109 [PMID:15686922] |
ChEMBL | Inhibition of HIV1 reverse transcriptase assessed as incorporation of biotin-dUTP into poly(rA)-oligo(dT) | B | 5.56 | pIC50 | 2740 | nM | IC50 | Eur J Med Chem (2012) 51: 60-66 [PMID:22405288] |
ChEMBL | Inhibition of recombinant wild type HIV1 RT using poly(rA)/oligo(dT)16 as template after 40 mins by spectrofluorometric analysis | B | 5.56 | pIC50 | 2740 | nM | IC50 | Eur J Med Chem (2013) 65: 134-143 [PMID:23707918] |
ChEMBL | Inhibition of purified recombinant HIV-1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation using poly(rC)-oligo(dG) as template primer | B | 5.56 | pIC50 | 2740 | nM | IC50 | Medchemcomm (2013) 4: 810-816 |
ChEMBL | Inhibition of HIV1 recombinant reverse transcriptase assessed as incorporation of biotin-dUTP into poly(rC)-oligo(dG) by colorimetric analysis | B | 5.57 | pIC50 | 2700 | nM | IC50 | Bioorg Med Chem (2012) 20: 6795-6802 [PMID:23098609] |
ChEMBL | Inhibition of HIV1 reverse transcriptase assessed as biotin-dUTP incorporation into enzyme using poly(rC)-oligo(dG) as template primer by colorimetric analysis | B | 5.57 | pIC50 | 2700 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 7155-7162 [PMID:23084898] |
ChEMBL | Inhibitory activity against HIV-1 Y181C Reverse transcriptase (RT) | B | 5.59 | pIC50 | 2600 | nM | IC50 | J Med Chem (1995) 38: 4830-4838 [PMID:7490732] |
ChEMBL | Compound was evaluated for inhibition of Y181C HIV type I reverse transcriptase. | B | 5.59 | pIC50 | 2600 | nM | IC50 | J Med Chem (1995) 38: 4839-4847 [PMID:7490733] |
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 | 5.59 | pIC50 | 2550 | nM | IC50 | Bioorg Med Chem (2014) 22: 1459-1467 [PMID:24457088] |
ChEMBL | Inhibition of HIV1 reverse transcriptase using Poly rC.dG template | B | 5.6 | pIC50 | 2500 | nM | IC50 | Eur J Med Chem (2007) 42: 993-1003 [PMID:17321639] |
ChEMBL | Inhibition of HIV1 reverse transcriptase assessed as inhibition of biotinylated dUTP incorporation after 1 hr by ELISA | B | 5.6 | pIC50 | 2500 | nM | IC50 | Bioorg Med Chem (2014) 22: 1863-1872 [PMID:24581546] |
ChEMBL | Inhibition of HIV1 reverse transcriptase assessed as reduction in biotin-labeled dUTP incorporation into DNA using poly(A) x oligo(dT)15 as template/primer after 1 hr by ELISA | B | 5.62 | pIC50 | 2400 | nM | IC50 | Eur J Med Chem (2015) 93: 330-337 [PMID:25707013] |
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 | 5.63 | pIC50 | 2320 | nM | IC50 | Eur J Med Chem (2017) 140: 383-391 [PMID:28987601] |
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 | 5.63 | pIC50 | 2320 | nM | IC50 | ACS Med Chem Lett (2018) 9: 334-338 [PMID:29670696] |
ChEMBL | Ability to inhibit HIV-1 IIIB reverse transcriptase catalyzed incorporation of tritiated thymidine triphosphate onto a biotinylated rN.dN template primer | B | 5.68 | pIC50 | 2110 | nM | IC50 | Bioorg Med Chem Lett (1992) 2: 1745-1750 |
ChEMBL | Inhibition of HIV1 reverse transcriptase V179D mutant | B | 5.7 | pIC50 | 2000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3935-3938 [PMID:21636271] |
ChEMBL | Inhibition of reverse transcriptase activity in HIV1 NL4-3 infected MT4 cells before dialysis | B | 5.7 | pIC50 | 2000 | nM | IC50 | Antimicrob Agents Chemother (2007) 51: 638-644 [PMID:17116672] |
ChEMBL | Inhibitory activity against HIV-1 Mutant Reverse transcriptase K103N | B | 5.72 | pIC50 | 1900 | nM | IC50 | J Med Chem (1998) 41: 2960-2971 [PMID:9685235] |
ChEMBL | Inhibitory concentration against mutant reverse transcriptase of K103N was determined which is in turn resistant to pyridinones | B | 5.72 | pIC50 | 1900 | nM | IC50 | J Med Chem (1995) 38: 4830-4838 [PMID:7490732] |
ChEMBL | Inhibitory activity against HIV-1 Mutant Reverse transcriptase K103N | B | 5.73 | pIC50 | 1850 | nM | IC50 | J Med Chem (1998) 41: 2972-2984 [PMID:9685236] |
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 | 5.75 | pIC50 | 1795 | nM | IC50 | Eur J Med Chem (2015) 97: 1-9 [PMID:25935383] |
ChEMBL | Inhibition of wild-type HIV1 reverse transcriptase p66/p51 after 40 mins by spectrophotometry | B | 5.75 | pIC50 | 1780 | nM | IC50 | Bioorg Med Chem (2014) 22: 2535-2541 [PMID:24680058] |
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 | 5.75 | pIC50 | 1780 | 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 | 5.75 | pIC50 | 1780 | nM | IC50 | Bioorg Med Chem (2013) 21: 6477-6483 [PMID:24055077] |
ChEMBL | Inhibition of HIV1 wild type p66/p51 reverse transcriptase | B | 5.77 | pIC50 | 1700 | nM | IC50 | J Med Chem (2007) 50: 2370-2384 [PMID:17458947] |
ChEMBL | Inhibition of RNA dependent DNA polymerase activity of HIV1 BH10 recombinant reverse transcriptase p66/p51 assessed as residual enzyme activity | B | 5.77 | pIC50 | 1700 | nM | IC50 | J Med Chem (2008) 51: 5702-5713 [PMID:18800765] |
ChEMBL | Inhibition of DNA polymerase activity of HIV1 reverse transcriptase | B | 5.77 | pIC50 | 1700 | nM | IC50 | J Med Chem (2007) 50: 2370-2384 [PMID:17458947] |
ChEMBL | Inhibition of HIV-1 reverse transcriptase assessed as inhibition of biotin dUTP incorporation by primer extension assay | B | 5.77 | pIC50 | 1700 | nM | IC50 | Bioorg Med Chem (2013) 21: 7398-7405 [PMID:24134904] |
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 | 5.78 | pIC50 | 1650 | nM | IC50 | Eur J Med Chem (2015) 102: 215-222 [PMID:26276435] |
ChEMBL | Inhibition of wild type recombinant HIV1 reverse transcriptase p66/p51 using poly(rA)/oligo(dT)16 as template/primer measured after 40 mins by picogreen dye-based spectrofluorometric method | B | 5.81 | pIC50 | 1550 | nM | IC50 | Bioorg Med Chem (2020) 28: 115431-115431 [PMID:32197813] |
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 | 5.81 | pIC50 | 1550 | nM | IC50 | Bioorg Med Chem (2017) 25: 3861-3870 [PMID:28559060] |
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 | 5.81 | pIC50 | 1550 | nM | IC50 | Bioorg Med Chem (2018) 26: 661-674 [PMID:29291935] |
ChEMBL | Inhibition of recombinant HIV1 Reverse transcriptase p66/p51 using poly (rA)-oligo (dT) as template primer after 40 mins by spectrofluorometric analysis | B | 5.82 | pIC50 | 1528 | nM | IC50 | Bioorg Med Chem (2015) 23: 6587-6593 [PMID:26385446] |
ChEMBL | Inhibitory activity against HIV-1 Mutant Reverse transcriptase P236L | B | 5.83 | pIC50 | 1480 | nM | IC50 | J Med Chem (1998) 41: 2972-2984 [PMID:9685236] |
ChEMBL | Inhibition of recombinant wild type HIV1 reverse transcriptase using DIG-labeled dUTP/biotin-labeled dUTP and dTTP as template and viral nucleotides assessed as decrease in biotin-dUTP incorporation after 1 hr by ELISA | B | 5.86 | pIC50 | 1390 | nM | IC50 | ACS Med Chem Lett (2017) 8: 1188-1193 [PMID:29152052] |
ChEMBL | Inhibition of HIV1 recombinant wild type reverse transcriptase p66/p51 using dsDNA by microplate reader based assay | B | 5.87 | pIC50 | 1350 | nM | IC50 | Bioorg Med Chem (2014) 22: 4658-4666 [PMID:25127466] |
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 | 5.87 | pIC50 | 1350 | nM | IC50 | Eur J Med Chem (2016) 121: 352-363 [PMID:27267005] |
ChEMBL | Compound was tested for inhibitory activity against HIV-1 mutant type reverse transcriptase (K103N) | B | 5.89 | pIC50 | 1300 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 2169-2172 [PMID:9873507] |
ChEMBL | Inhibition of HIV 1 reverse transcriptase assessed as incorporation of biotin-dUTP into poly rA.dT by ELISA | B | 5.92 | pIC50 | 1200 | nM | IC50 | Bioorg Med Chem (2013) 21: 2128-2134 [PMID:23415090] |
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 | 5.94 | pIC50 | 1150 | nM | IC50 | Bioorg Med Chem (2015) 23: 1069-1081 [PMID:25638501] |
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 | 5.95 | pIC50 | 1130 | nM | IC50 | Bioorg Med Chem (2017) 25: 3861-3870 [PMID:28559060] |
ChEMBL | Covalent inhibition of recombinant wild type HIV-1 reverse transcriptase using poly(rA)350/oligo(dT)16 as template/primer preincubated followed by substrate addition measured after 1 hr by pico-green reagent based fluorescence analysis | B | 5.97 | pIC50 | 1060 | nM | IC50 | ACS Med Chem Lett (2021) 12: 249-255 [PMID:33603971] |
ChEMBL | Inhibition of wild type HIV1 p66/p51 reverse transcriptase by spectrofluorometry | B | 6 | pIC50 | 1000 | nM | IC50 | Bioorg Med Chem (2015) 23: 624-631 [PMID:25537532] |
ChEMBL | Inhibition of HIV1 reverse transcriptase using 234-nt long RNA/18-mer DNA oligonucleotide as template/primer preincubated for 15 mins followed by incubation with template/primer for 40 mins by liquid scintillation counting in presence of alpha[P33]-dCTP | B | 6.04 | pIC50 | 920 | nM | IC50 | Bioorg Med Chem (2016) 24: 2519-2529 [PMID:27108399] |
ChEMBL | Inhibition of HIV1 wild type reverse transcriptase p66/p51 using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry | B | 6.04 | pIC50 | 910 | nM | IC50 | Bioorg Med Chem (2016) 24: 2476-2485 [PMID:27112451] |
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 | 6.05 | pIC50 | 900 | nM | IC50 | Bioorg Med Chem (2018) 26: 2051-2060 [PMID:29559197] |
ChEMBL | Inhibition of HIV1 RT mediated DNA-dependent DNA synthesis initiation using RNA PPT primed substrate by scintillation proximity assay | B | 6.05 | pIC50 | 900 | nM | IC50 | J Biol Chem (2007) 282: 8005-8010 [PMID:17172472] |
ChEMBL | Inhibition of HIV1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation using hybrid poly (A).oligo (dT)15 template primer incubated for 1 hr at 37 degC by ELISA method | B | 6.05 | pIC50 | 900 | nM | IC50 | Bioorg Med Chem (2014) 22: 5290-5297 [PMID:25150090] |
ChEMBL | Inhibition of wild type HIV-1 reverse transcriptase assessed as assessed as inhibition of biotin deoxyuridine triphosphate incorporation into protein | B | 6.05 | pIC50 | 890 | nM | IC50 | Eur J Med Chem (2023) 247: 115042-115042 [PMID:36577220] |
ChEMBL | Inhibition of HIV1 reverse transcriptase Y188C mutant in 293T cells | B | 6.07 | pIC50 | 860 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 3034-3038 [PMID:16527484] |
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 | 6.07 | pIC50 | 860 | nM | IC50 | Eur J Med Chem (2021) 226: 113868-113868 [PMID:34583311] |
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 | 6.09 | pIC50 | 807 | nM | IC50 | Bioorg Med Chem (2015) 23: 4248-4255 [PMID:26162497] |
ChEMBL | Inhibition of wild type HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation into protein incubated for 1 hrs by ELISA | B | 6.11 | pIC50 | 778 | nM | IC50 | J Med Chem (2021) 64: 13658-13675 [PMID:34432448] |
ChEMBL | Inhibition of wild type HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation into protein incubated for 1 hrs by ELISA | B | 6.11 | pIC50 | 778 | nM | IC50 | J Med Chem (2021) 64: 13658-13675 [PMID:34432448] |
ChEMBL | Inhibition of recombinant wild-type p66/p51 HIV-1 reverse transcriptase incubated for 40 mins by picogreen dye-based spectrofluorometric analysis | B | 6.15 | pIC50 | 705 | nM | IC50 | Eur J Med Chem (2022) 238: 114512-114512 [PMID:35679690] |
ChEMBL | Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase DNA-dependent DNA polymerase activity by gel-based primer extension assay | B | 6.15 | pIC50 | 700 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 4667-4672 [PMID:19704127] |
ChEMBL | Inhibition of HIV1 reverse transcriptase assessed as residual enzyme activity at 50 uM after 1 hr by ELISA | B | 6.17 | pIC50 | 670 | nM | IC50 | Bioorg Med Chem (2011) 19: 4227-4237 [PMID:21700466] |
ChEMBL | Inhibition of wild-type HIV1 reverse transcriptase assessed as incorporation of biotin-labeled dUTP | B | 6.17 | pIC50 | 670 | nM | IC50 | Bioorg Med Chem (2014) 22: 633-642 [PMID:24275349] |
ChEMBL | Inhibition of HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation into template incubated for 1 hr by ELISA | B | 6.19 | pIC50 | 645.65 | 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 | 6.19 | pIC50 | 640 | nM | IC50 | Eur J Med Chem (2021) 213: 113051-113051 [PMID:33279288] |
ChEMBL | Inhibition of wild type HIV-1 reverse transcriptase assessed as reduction of biotin-dUTP incorporation into protein using ABTS as substrate incubated for 1 hrs by ELISA analysis | B | 6.2 | pIC50 | 638 | nM | IC50 | Eur J Med Chem (2023) 246: 114957-114957 [PMID:36446205] |
ChEMBL | Inhibition of DNA dependent DNA polymerase activity of HIV1 BH10 recombinant reverse transcriptase p66/p51 assessed as residual enzyme activity | B | 6.2 | pIC50 | 630 | nM | IC50 | J Med Chem (2008) 51: 5702-5713 [PMID:18800765] |
ChEMBL | HIV-1 reverse transcriptase inhibitory activity against Asn103 mutant using (poly)rC600*(oligo)dGT as template primer. | B | 6.2 | pIC50 | 625 | nM | IC50 | J Med Chem (1999) 42: 4150-4160 [PMID:10514285] |
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 | 6.21 | pIC50 | 620 | nM | IC50 | Eur J Med Chem (2014) 87: 52-62 [PMID:25240095] |
ChEMBL | Inhibition of wild-type HIV1 Reverse transcriptase p66/p51 assessed as relative fluorescence signal after 40 mins | B | 6.21 | pIC50 | 620 | nM | IC50 | Bioorg Med Chem (2015) 23: 3860-3868 [PMID:25907370] |
ChEMBL | Inhibitory activity against HIV rRT activity in wild type IIIB strain | B | 6.22 | pIC50 | 600 | nM | IC50 | J Med Chem (1996) 39: 522-530 [PMID:8558522] |
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 | 6.23 | pIC50 | 595 | 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 | 6.23 | pIC50 | 595 | nM | IC50 | Bioorg Med Chem (2019) 27: 447-456 [PMID:30606670] |
ChEMBL | Inhibition of wild-type HIV1 reverse transcriptase infected in human MT4 cells assessed as reduction in biotin-dUTP incorporation | B | 6.23 | pIC50 | 590 | nM | IC50 | ACS Med Chem Lett (2018) 9: 370-375 [PMID:29670703] |
ChEMBL | Inhibition of HIV1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation into template incubated for 1 hr by ELISA | B | 6.23 | pIC50 | 590 | nM | IC50 | Eur J Med Chem (2019) 182: 111619-111619 [PMID:31434039] |
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 | 6.23 | pIC50 | 588.84 | nM | IC50 | J Med Chem (2019) 62: 2083-2098 [PMID:30721060] |
ChEMBL | Inhibition of HIV1 reverse transcriptase assessed as reduction in biotin-labeled dUTP incorporation into DNA after 1 hr using poly(A) x oligo(dT)15 template/primer hybrid, digoxigenin and biotin-labeled nucleotides | B | 6.24 | pIC50 | 580 | nM | IC50 | Eur J Med Chem (2015) 92: 754-765 [PMID:25626145] |
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 | 6.24 | pIC50 | 580 | nM | IC50 | J Med Chem (2021) 64: 10297-10311 [PMID:34197708] |
ChEMBL | Inhibition of recombinant wild type p66/p51 HIV1 reverse transcriptase incubated for 40 mins by picogreen dye-based spectrofluorometric analysis | B | 6.24 | pIC50 | 580 | nM | IC50 | J Med Chem (2021) 64: 5067-5081 [PMID:33851529] |
ChEMBL | Inhibition of recombinant wild type p66/p51 HIV1 reverse transcriptase incubated for 40 mins by picogreen dye-based spectrofluorometric analysis | B | 6.24 | pIC50 | 580 | nM | IC50 | J Med Chem (2022) 65: 2122-2138 [PMID:35073089] |
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 | 6.24 | pIC50 | 575 | nM | IC50 | Eur J Med Chem (2021) 214: 113204-113204 [PMID:33567378] |
ChEMBL | Inhibition of recombinant HIV-1 BH10 reverse transcriptase p51/p66 expressed in Escherichia coli preincubated for 10 mins followed by D38/25PGA template-primer addition and measured after 10 to 30 secs by denaturing PAGE based single nucleotide incorporation assay | B | 6.24 | pIC50 | 570 | nM | IC50 | ACS Med Chem Lett (2020) 11: 811-817 [PMID:32435389] |
ChEMBL | Inhibition of HIV-1 reverse transcriptase using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorometric analysis | B | 6.26 | pIC50 | 552 | nM | IC50 | J Med Chem (2022) 65: 8478-8492 [PMID:35649164] |
ChEMBL | Inhibition of recombinant HIV1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation in to poly [A] x oligo[dT]15 by ELISA | B | 6.26 | pIC50 | 550 | nM | IC50 | Bioorg Med Chem (2014) 22: 2052-2059 [PMID:24631361] |
ChEMBL | Inhibition of recombinant HIV1 reverse transcriptase using poly rA:dT as template/primer after 1 hr by ELISA | B | 6.29 | pIC50 | 510 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 6593-6597 [PMID:24239481] |
ChEMBL | Inhibition of recombinant wild type HIV1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation into template | B | 6.29 | pIC50 | 510 | nM | IC50 | J Med Chem (2021) 64: 4239-4256 [PMID:33734714] |
ChEMBL | Compound was tested for Inhibition of HIV-1 RT activity. | B | 6.3 | pIC50 | 500 | nM | IC50 | J Med Chem (1996) 39: 2672-2680 [PMID:8709096] |
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 | 6.3 | pIC50 | 500 | nM | IC50 | Med Chem Res (2006) 15: 492-510 |
ChEMBL | Inhibition of recombinant HIV1 reverse transcriptase by colorimetric assay | B | 6.3 | pIC50 | <500 | nM | IC50 | Eur J Med Chem (2021) 224: 113681-113681 [PMID:34246921] |
ChEMBL | Inhibition of HIV-1 reverse transcriptase using [2,8-3H]dGTP as substrate by fluorescence based assay | B | 6.31 | pIC50 | 490 | nM | IC50 | Eur J Med Chem (2023) 248: 115114-115114 [PMID:36640458] |
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 | 6.32 | pIC50 | 480 | nM | IC50 | Eur J Med Chem (2021) 226: 113868-113868 [PMID:34583311] |
ChEMBL | Inhibition of HIV1 RT mediated DNA-dependent DNA synthesis initiation using RNA/DNAM duplex primed substrate by scintillation proximity assay | B | 6.35 | pIC50 | 450 | nM | IC50 | J Biol Chem (2007) 282: 8005-8010 [PMID:17172472] |
ChEMBL | Inhibitory activity against HIV-1 reverse transcriptase (HIV-RT) | B | 6.37 | pIC50 | 430 | nM | IC50 | J Med Chem (1993) 36: 2526-2535 [PMID:7689109] |
ChEMBL | In vitro for inhibitory activity against HIV-1 Reverse Transcriptase | B | 6.37 | pIC50 | 430 | nM | IC50 | J Med Chem (1993) 36: 726-732 [PMID:7681480] |
ChEMBL | Inhibition of recombinant wild type HIV1 reverse transcriptase p66/p51 incubated for 40 mins by picogreen dye-based spectrofluorometric analysis | B | 6.39 | pIC50 | 404 | 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 | 6.39 | pIC50 | 404 | nM | IC50 | Eur J Med Chem (2019) 182: 111603-111603 [PMID:31421633] |
ChEMBL | Inhibition of recombinant wild type HIV-1 reverse transcriptase using DNA/RNA as substrate incubated for 40 mins by Pico-green dye based spectrofluorometric analysis | B | 6.39 | pIC50 | 404 | nM | IC50 | J Med Chem (2023) 66: 4755-4767 [PMID:36996328] |
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 | 6.4 | pIC50 | 400 | nM | IC50 | Eur J Med Chem (2020) 208: 112696-112696 [PMID:32883642] |
ChEMBL | Inhibition of HIV1 wild type reverse transcriptase | B | 6.4 | pIC50 | 400 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3935-3938 [PMID:21636271] |
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 | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (2012) 55: 6634-6638 [PMID:22712652] |
ChEMBL | Inhibition of HIV1 wild-type reverse transcriptase using [3H]dTTP by scintillation counting | B | 6.4 | pIC50 | 400 | nM | IC50 | Eur J Med Chem (2014) 80: 101-111 [PMID:24769348] |
ChEMBL | Inhibition of wild type HIV1 reverse transcriptase 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 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 | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (2017) 60: 6528-6547 [PMID:28628334] |
ChEMBL | Inhibition of HIV1 Reverse transcriptase incubated for 30 mins by fluorescence based analysis | B | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (2023) 66: 6193-6217 [PMID:37130343] |
ChEMBL | Inhibition of wild type HIV-1 reverse transcriptase assessed as inhibition of biotin deoxyuridine triphosphate incorporation into protein | B | 6.42 | pIC50 | 380 | nM | IC50 | Eur J Med Chem (2023) 246: 114939-114939 [PMID:36442370] |
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 | 6.49 | pIC50 | 323 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 3491-3495 [PMID:30318436] |
ChEMBL | In vitro inhibition of mutant P236L recombinant reverse transcriptase of HIV-1 IIIB | B | 6.49 | pIC50 | 320 | nM | IC50 | J Med Chem (1996) 39: 3769-3789 [PMID:8809165] |
ChEMBL | In vitro ability to inhibit mutant P236L reverse transcriptase | B | 6.49 | pIC50 | 320 | nM | IC50 | J Med Chem (2000) 43: 1034-1040 [PMID:10715167] |
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 | 6.49 | pIC50 | 320 | nM | IC50 | Eur J Med Chem (2020) 185: 111874-111874 [PMID:31735575] |
ChEMBL | Inhibition of HIV-1 reverse transcriptase assessed as assessed as reduction of biotin-dUTP incorporation into protein incubated for 1 hrs by ELISA analysis | B | 6.5 | pIC50 | 315 | nM | IC50 | J Med Chem (2023) 66: 8643-8665 [PMID:37255025] |
ChEMBL | Inhibitory activity against HIV-1 recombinant reverse transcriptase. | B | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (2001) 44: 2544-2554 [PMID:11472208] |
ChEMBL | Concentration required for 50% inhibition of wild type human immunodeficiency virus type 1 reverse transcriptase | B | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (2004) 47: 5912-5922 [PMID:15537346] |
ChEMBL | Concentration required to inhibit the HIV-1 reverse transcriptase activity by 50%. | B | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (1999) 42: 619-627 [PMID:10052969] |
ChEMBL | Inhibition of reverse transcriptase activity of HIV-1 in the presence of [alpha35 S] TTP as cosubstrate | B | 6.55 | pIC50 | 280 | nM | IC50 | J Med Chem (1993) 36: 3784-3794 [PMID:7504733] |
ChEMBL | Compound concentration required to inhibit the HIV-1 recombinant Reverse transcriptase (rRT) activity by 50%. | B | 6.57 | pIC50 | 270 | nM | IC50 | J Med Chem (1997) 40: 1447-1454 [PMID:9154967] |
ChEMBL | Inhibition of HIV1 reverse transcriptase | B | 6.6 | pIC50 | 250 | nM | IC50 | Eur J Med Chem (2011) 46: 106-121 [PMID:21093117] |
ChEMBL | Concentration required to protect the cell against HIV-1 strain IIIB viral cytopathogenicity by 50% in MT-4 cells | F | 6.6 | pIC50 | 250 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 3173-3176 [PMID:15149669] |
ChEMBL | Inhibition of HIV-1 recombinant reverse transcriptase | B | 6.6 | pIC50 | 250 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 1931-1936 |
ChEMBL | Inhibitory concentration against wild-type reverse transcriptase of HIV-1 | B | 6.64 | pIC50 | 230 | nM | IC50 | J Med Chem (2004) 47: 1175-1182 [PMID:14971897] |
ChEMBL | Tested for inhibitory concentration on HIV-1 Reverse transcriptase in the presence of poly(c)-oligo-(dG) | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2000) 43: 3949-3962 [PMID:11052800] |
ChEMBL | Inhibition of HIV-1 reverse transcriptase using rCdG as template and dGTP as substrate | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (1995) 38: 4929-4936 [PMID:8523406] |
ChEMBL | Inhibitory effect on wild type HIV- 1 reverse transcriptase using rCdG as template and dGTP as substrate. | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 1511-1516 [PMID:9873380] |
ChEMBL | Tested for the inhibition of wild type HIV-1 (IIIB) RT | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (1996) 39: 4261-4274 [PMID:8863804] |
ChEMBL | Inhibition of recombinant HIV-1 reverse transcriptase incubated for 2 hrs by colorimetric assay | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2021) 64: 16530-16540 [PMID:34735153] |
ChEMBL | Inhibition of recombinant HIV-1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation in to cDNA chain incubated for 1 hr by ELISA | B | 6.74 | pIC50 | 181 | nM | IC50 | J Med Chem (2020) 63: 1298-1312 [PMID:31935327] |
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 | 6.74 | pIC50 | 180 | nM | IC50 | Bioorg Med Chem (2009) 17: 5962-5967 [PMID:19616956] |
ChEMBL | Compound was tested for inhibitory activity against HIV-1 mutant type reverse transcriptase (P236L) | B | 6.74 | pIC50 | 180 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 2169-2172 [PMID:9873507] |
ChEMBL | Inhibition of RNA-dependent DNA polymerase activity of HIV1 reverse transcriptase using poly(rA)/pligo(dT) template | B | 6.74 | pIC50 | 180 | nM | IC50 | Bioorg Med Chem (2010) 18: 1702-1710 [PMID:20097079] |
ChEMBL | Inhibition of HIV1 reverse transcriptase RNA-dependent DNA polymerase activity assessed as incorporation of radioactive dTTP into poly(rA)/oligo(DT) | B | 6.74 | pIC50 | 180 | nM | IC50 | Bioorg Med Chem (2008) 16: 7429-7435 [PMID:18585918] |
ChEMBL | Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase | B | 6.74 | pIC50 | 180 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 1956-1960 [PMID:17276064] |
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 | 6.75 | pIC50 | 176 | nM | IC50 | Eur J Med Chem (2018) 145: 726-734 [PMID:29353724] |
ChEMBL | Compound was tested for inhibitory activity against HIV-1 mutant type reverse transcriptase (L1001) | B | 6.77 | pIC50 | 170 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 2169-2172 [PMID:9873507] |
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 | 6.8 | pIC50 | 160 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 4101-4105 [PMID:27390064] |
ChEMBL | Inhibition of HIV1 isolate R8 reverse transcriptase after 90 mins | B | 6.86 | pIC50 | 137 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 2424-2431 [PMID:19289522] |
ChEMBL | Inhibitory concentration against mutant reverse transcriptase of L100I was determined which is in turn resistant TIBO | B | 6.89 | pIC50 | 130 | nM | IC50 | J Med Chem (1995) 38: 4830-4838 [PMID:7490732] |
ChEMBL | HIV-1 reverse transcriptase inhibitory activity against Ile 100 mutant using (poly)rC600*(oligo)dGT as template primer. | B | 6.89 | pIC50 | 130 | nM | IC50 | J Med Chem (1999) 42: 4150-4160 [PMID:10514285] |
ChEMBL | Inhibition of recombinant HIV1 His-tagged p66/p51 reverse transcriptase expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)-oligo(dT) (12 to 18 bp) as template/primer incubated for 20 mins by scintillation counting method | B | 6.9 | pIC50 | 125 | nM | IC50 | J Med Chem (2016) 59: 2747-2759 [PMID:26898379] |
ChEMBL | HIV-1 reverse transcriptase inhibitory activity against Cys181 mutant using (poly)rC600*(oligo)dGT as template primer. | B | 6.94 | pIC50 | 114 | nM | IC50 | J Med Chem (1999) 42: 4150-4160 [PMID:10514285] |
ChEMBL | Inhibitory concentration against mutant reverse transcriptase of E138K was determined which is in turn resistant to TSAO | B | 6.96 | pIC50 | 110 | nM | IC50 | J Med Chem (1995) 38: 4830-4838 [PMID:7490732] |
ChEMBL | Inhibition of wild-type HIV1 reverse transcriptase in HIV1 infected HEK293T cells harboring luciferase gene assessed as reduction in viral infection after 48 hrs by Bright-Glo luciferase assay | B | 6.98 | pIC50 | 105 | nM | IC50 | ACS Med Chem Lett (2019) 10: 196-202 [PMID:30783503] |
ChEMBL | Inhibition of HIV1 reverse transcriptase using T19-Cy5 labeled 23-mer DNA/T2-TAMRA labeled 63-mer DNA as primer/template assessed as inhibition of dNTP incorporation into primer/template | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2016) 59: 7212-7222 [PMID:27339173] |
ChEMBL | Inhibition of HIV1 reverse transcriptase derived from HIV patient plasma by LC/MS/MS analysis | B | 7.08 | pIC50 | 84 | nM | IC50 | J Med Chem (2019) 62: 4851-4883 [PMID:30516990] |
ChEMBL | Inhibition of HIV1 reverse transcriptase | B | 7.08 | pIC50 | 84 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 469-473 [PMID:18083556] |
ChEMBL | In vitro for inhibition of HIV-1 reverse transcriptase. | B | 7.08 | pIC50 | 84 | nM | IC50 | J Med Chem (1995) 38: 1406-1410 [PMID:7537334] |
ChEMBL | In vitro inhibitory activity against human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) | B | 7.08 | pIC50 | 84 | nM | IC50 | J Med Chem (1991) 34: 2231-2241 [PMID:1712395] |
ChEMBL | Inhibition of HIV-1 reverse transcriptase at 37 degree Centigrade | B | 7.08 | pIC50 | 84 | nM | IC50 | J Med Chem (2001) 44: 145-154 [PMID:11170624] |
ChEMBL | Inhibition of HIV1 reverse transcriptase | B | 7.08 | pIC50 | 84 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1530-1533 [PMID:18222088] |
ChEMBL | Inhibitory activity against HIV-1 Reverse transcriptase (RT) was determined | B | 7.08 | pIC50 | 84 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 163-166 |
ChEMBL | Compound was evaluated for inhibition of WT HIV type I reverse transcriptase. | B | 7.1 | pIC50 | 80 | nM | IC50 | J Med Chem (1995) 38: 4839-4847 [PMID:7490733] |
ChEMBL | Inhibitory activity against HIV-1 Mutant Reverse transcriptase P236L | B | 7.1 | pIC50 | 80 | nM | IC50 | J Med Chem (1998) 41: 2960-2971 [PMID:9685235] |
ChEMBL | Inhibitory activity against HIV-1 Mutant Reverse transcriptase G190A | B | 7.1 | pIC50 | 80 | nM | IC50 | J Med Chem (1998) 41: 2972-2984 [PMID:9685236] |
ChEMBL | Inhibitory concentration against HIV-1 wild type Reverse transcriptase (RT) | B | 7.1 | pIC50 | 80 | nM | IC50 | J Med Chem (1995) 38: 4830-4838 [PMID:7490732] |
ChEMBL | Inhibitory concentration against mutant reverse transcriptase of P236L was determined which is in turn resistant to BHAP | B | 7.1 | pIC50 | 80 | nM | IC50 | J Med Chem (1995) 38: 4830-4838 [PMID:7490732] |
ChEMBL | Ability to inhibit HIV-1 Reverse Transcriptase (RT) using an rC-dG template/primer | B | 7.14 | pIC50 | 73 | nM | IC50 | J Med Chem (1994) 37: 2437-2444 [PMID:7520079] |
ChEMBL | In vitro inhibitory concentration against HIV-1 reverse transcriptase using rC-dG template primer | B | 7.14 | pIC50 | 73 | nM | IC50 | J Med Chem (1993) 36: 249-255 [PMID:7678654] |
ChEMBL | Inhibition of wild type HIV1 reverse transcriptase in 293T cells | B | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 3034-3038 [PMID:16527484] |
ChEMBL | Compound was tested for inhibitory activity against HIV-1 wild type reverse transcriptase | B | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 2169-2172 [PMID:9873507] |
ChEMBL | Inhibition of reverse transcriptase activity in HIV1 infected HeLa-MAGI cells at 37 deg C after 48 hrs | B | 7.3 | pIC50 | 50 | nM | IC50 | Antimicrob Agents Chemother (2007) 51: 638-644 [PMID:17116672] |
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 | 8.72 | pIC50 | 1.9 | nM | IC50 | Eur J Med Chem (2019) 176: 11-20 [PMID:31091477] |
ChEMBL | HIV-1 reverse transcriptase inhibitory activity against Wild Type Reverse transcriptase using (poly)rC600*(oligo)dGT as template primer. | B | 8.89 | pIC50 | 1.3 | nM | IC50 | J Med Chem (1999) 42: 4150-4160 [PMID:10514285] |
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 | 4.82 | pEC50 | >15020 | nM | EC50 | ACS Med Chem Lett (2018) 9: 370-375 [PMID:29670703] |
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 | 4.82 | pEC50 | >15000 | nM | EC50 | J Med Chem (2017) 60: 4424-4443 [PMID:28481112] |
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 | 4.82 | pEC50 | >15000 | nM | EC50 | Bioorg Med Chem (2018) 26: 661-674 [PMID:29291935] |
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 | 4.82 | pEC50 | >15000 | 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 | 4.82 | pEC50 | >15000 | nM | EC50 | Bioorg Med Chem (2018) 26: 661-674 [PMID:29291935] |
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 | 4.82 | pEC50 | >15000 | nM | EC50 | Bioorg Med Chem (2018) 26: 661-674 [PMID:29291935] |
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 | 4.82 | pEC50 | >15000 | nM | EC50 | Bioorg Med Chem (2017) 25: 2491-2497 [PMID:28314514] |
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 | 4.82 | pEC50 | >15000 | nM | EC50 | J Med Chem (2017) 60: 4424-4443 [PMID:28481112] |
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 | 4.82 | pEC50 | >15000 | nM | EC50 | J Med Chem (2017) 60: 4424-4443 [PMID:28481112] |
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 | 4.82 | pEC50 | >15000 | nM | EC50 | J Med Chem (2017) 60: 4424-4443 [PMID:28481112] |
ChEMBL | Inhibition of HIV RT K103N/Y181C mutant by cell based assay | B | 5 | pEC50 | >10000 | nM | EC50 | Eur J Med Chem (2013) 65: 134-143 [PMID:23707918] |
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 | 5.02 | pEC50 | 9590 | nM | EC50 | Bioorg Med Chem (2018) 26: 661-674 [PMID:29291935] |
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 | 5.04 | pEC50 | 9074 | nM | EC50 | Eur J Med Chem (2021) 214: 113204-113204 [PMID:33567378] |
ChEMBL | Inhibition of HIV-1 p66/p51 reverse transcriptase Y181C mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis | B | 5.09 | pEC50 | 8082 | nM | EC50 | J Med Chem (2021) 64: 5067-5081 [PMID:33851529] |
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 | 5.09 | pEC50 | 8041 | nM | EC50 | Eur J Med Chem (2021) 214: 113204-113204 [PMID:33567378] |
ChEMBL | Inhibition of HIV-1 p66/p51 reverse transcriptase K103N mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis | B | 5.1 | pEC50 | 8026 | nM | EC50 | J Med Chem (2021) 64: 5067-5081 [PMID:33851529] |
ChEMBL | Antiviral activity against HIV1 Y188L mutant in MT4 cells by MTT assay | F | 5.12 | pEC50 | >7500 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 3541-3544 [PMID:16621553] |
ChEMBL | Antiviral activity against HIV1 IRLL98 in MT4 cells by MTT assay | F | 5.12 | pEC50 | >7500 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 3541-3544 [PMID:16621553] |
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 | 5.19 | pEC50 | 6496.4 | nM | EC50 | Eur J Med Chem (2020) 202: 112549-112549 [PMID:32712537] |
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 | 5.27 | pEC50 | 5390 | nM | EC50 | J Med Chem (2017) 60: 4424-4443 [PMID:28481112] |
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 | 5.33 | pEC50 | 4694 | nM | EC50 | Eur J Med Chem (2020) 202: 112549-112549 [PMID:32712537] |
ChEMBL | Inhibition of HIV-1 p66/p51 reverse transcriptase L100I mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis | B | 5.39 | pEC50 | 4106 | nM | EC50 | J Med Chem (2021) 64: 5067-5081 [PMID:33851529] |
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 | 5.41 | pEC50 | 3922 | nM | EC50 | Eur J Med Chem (2021) 214: 113204-113204 [PMID:33567378] |
ChEMBL | Antiviral activity against HIV1 K103N mutant in MT4 cells by MTT assay | F | 5.41 | pEC50 | 3900 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 3541-3544 [PMID:16621553] |
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 | 5.5 | pEC50 | 3154.3 | nM | EC50 | Eur J Med Chem (2020) 202: 112549-112549 [PMID:32712537] |
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 | 5.68 | pEC50 | 2100 | nM | EC50 | J Med Chem (2017) 60: 4424-4443 [PMID:28481112] |
ChEMBL | Inhibition of HIV-1 reverse transcriptase after 1 hr by spectrophotometry | B | 5.77 | pEC50 | 1700 | nM | EC50 | J Nat Prod (2013) 76: 2298-2306 [PMID:24308675] |
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 | 5.92 | pEC50 | 1201.7 | 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 | 6.21 | pEC50 | 622 | nM | EC50 | Eur J Med Chem (2021) 214: 113204-113204 [PMID:33567378] |
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 | 6.35 | pEC50 | 450 | nM | EC50 | Bioorg Med Chem (2018) 26: 661-674 [PMID:29291935] |
ChEMBL | Effective concentration required against L100I mutant HIV-1 reverse transcriptase (as per ref 8 in the article) | B | 6.42 | pEC50 | 380 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 2799-2802 [PMID:11597403] |
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 | 6.57 | pEC50 | 271 | nM | EC50 | J Med Chem (2017) 60: 4424-4443 [PMID:28481112] |
ChEMBL | Concentration required to inhibit HIV-1 reverse transcriptase activity (wild-type) by 50% | B | 6.6 | pEC50 | 250 | nM | EC50 | J Med Chem (2005) 48: 4378-4388 [PMID:15974590] |
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 | 6.62 | pEC50 | 240 | nM | EC50 | Bioorg Med Chem (2017) 25: 2491-2497 [PMID:28314514] |
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 | 6.77 | pEC50 | 168 | nM | EC50 | Eur J Med Chem (2021) 214: 113204-113204 [PMID:33567378] |
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 | 6.91 | pEC50 | 124 | nM | EC50 | ACS Med Chem Lett (2018) 9: 370-375 [PMID:29670703] |
ChEMBL | Effective concentration required against wild type HIV-1 reverse transcriptase (as per ref 6 in the article) | B | 6.96 | pEC50 | 110 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 2799-2802 [PMID:11597403] |
ChEMBL | Effective concentration required against L100I mutant HIV-1 reverse transcriptase (as per ref 12 in the article) | B | 7 | pEC50 | 100 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 2799-2802 [PMID:11597403] |
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 | 7.12 | pEC50 | 75 | nM | EC50 | Bioorg Med Chem (2018) 26: 661-674 [PMID:29291935] |
ChEMBL | Effective concentration required against L100I mutant HIV-1 reverse transcriptase (as per ref 6 in the article) | B | 7.15 | pEC50 | 70 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 2799-2802 [PMID:11597403] |
ChEMBL | Effective concentration required against L100I mutant HIV-1 reverse transcriptase (as per ref 7 in the article) | B | 7.28 | pEC50 | 53 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 2799-2802 [PMID:11597403] |
ChEMBL | Antiviral activity against wild type HIV1 NL4-3 in MT4 cells by MTT assay | F | 7.28 | pEC50 | 52 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 3541-3544 [PMID:16621553] |
ChEMBL | Effective concentration required against wild type HIV-1 reverse transcriptase (as per ref 8 in the article) | B | 7.52 | pEC50 | 30 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 2799-2802 [PMID:11597403] |
ChEMBL | Effective concentration required against wild type HIV-1 reverse transcriptase (as per ref 7 in the article) | B | 7.59 | pEC50 | 26 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 2799-2802 [PMID:11597403] |
ChEMBL | Effective concentration required against wild type HIV-1 reverse transcriptase (as per ref 12 in the article) | B | 7.7 | pEC50 | 20 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 2799-2802 [PMID:11597403] |
ChEMBL | Inhibition of HIV1 reverse transcriptase by EIA | B | 8.44 | pEC50 | 3.6 | nM | EC50 | Bioorg Med Chem (2010) 18: 2029-2036 [PMID:20137956] |
Human immunodeficiency virus type 2 pol protein in Human immunodeficiency virus 2 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5074] [UniProtKB: P88142] | ||||||||
ChEMBL | Inhibitory activity against HIV rRT activity in HIV-2 | B | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (1996) 39: 522-530 [PMID:8558522] |
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human O positive erythrocyte assessed as reduction in parasitemia after 72 hrs | F | 4.19 | pIC50 | 64000 | nM | IC50 | Bioorg Med Chem (2014) 22: 5241-5248 [PMID:25199582] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]