etravirine [Ligand Id: 12675] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL308954 (Etravirina, Etravirine, Intelence, R-165335, R165335, TMC 125, TMC-125, TMC125) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0] | ||||||||
| ChEMBL | Inhibition of BCRP expressed in MDCK2 cells assessed as cell growth inhibition by calcein and pheophorbide A efflux assays | B | 5.22 | pIC50 | 6000 | nM | IC50 | Antimicrob Agents Chemother (2011) 55: 1282-1284 [PMID:21189339] |
| ABCC2/Canalicular multispecific organic anion transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5748] [GtoPdb: 780] [UniProtKB: Q92887] | ||||||||
| ChEMBL | Inhibition of MRP2 expressed in MDCK2 cells assessed as cell growth inhibition by calcein and pheophorbide A efflux assays | B | 5.11 | pIC50 | 7800 | nM | IC50 | Antimicrob Agents Chemother (2011) 55: 1282-1284 [PMID:21189339] |
| ABCC3/Canalicular multispecific organic anion transporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5918] [GtoPdb: 781] [UniProtKB: O15438] | ||||||||
| ChEMBL | Inhibition of MRP3 expressed in MDCK2 cells assessed as cell growth inhibition by calcein and pheophorbide A efflux assays | B | 5.29 | pIC50 | 5100 | nM | IC50 | Antimicrob Agents Chemother (2011) 55: 1282-1284 [PMID:21189339] |
| Cruzipain in Trypanosoma cruzi (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3563] [UniProtKB: P25779] | ||||||||
| ChEMBL | Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in absence of Triton X-100 | B | 5.4 | pIC50 | 4000 | nM | IC50 | J Med Chem (2010) 53: 4259-4265 [PMID:20426472] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) cells stable expressing hERG measured using IonWorks Barracuda automated patch clamp platform | F | 4.6 | pIC50 | 25118.86 | nM | IC50 | J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753] |
| Human immunodeficiency virus type 1 reverse transcriptase in Human immunodeficiency virus 1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL247] [UniProtKB: Q72547] | ||||||||
| ChEMBL | Binding affinity to HIV-1 reverse transcriptase assessed as dissociation constant by SPR analysis | B | 5.84 | pKd | 1460 | nM | Kd | J Med Chem (2022) 65: 15608-15626 [PMID:36411036] |
| ChEMBL | Inhibition of wild type HIV-1 reverse transcriptase using poly (rC)/oligo (dG) as template/primer assessed as inhibition of biotin-dUTP incorporation after 1 hr by microtiter plate ELISA reader analysis | B | 5.19 | pIC50 | 6500 | nM | IC50 | Eur J Med Chem (2014) 76: 531-538 [PMID:24602795] |
| 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 | 5.51 | pIC50 | 3100 | nM | IC50 | Bioorg Med Chem (2016) 24: 4424-4433 [PMID:27501911] |
| 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 | 5.51 | pIC50 | 3100 | 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 | 5.51 | pIC50 | 3100 | nM | IC50 | Eur J Med Chem (2016) 109: 294-304 [PMID:26802545] |
| ChEMBL | Inhibition of DNA-dependent DNA polymerase activity of HIV1 subtype B reverse transcriptase M230L mutant by gel-based primer extension assay | B | 5.88 | pIC50 | 1320 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 2401-2408 [PMID:20308384] |
| 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 | 6 | pIC50 | 1000 | nM | IC50 | ACS Med Chem Lett (2017) 8: 1188-1193 [PMID:29152052] |
| ChEMBL | Inhibition of HIV1 wildtype reverse transcriptase using poly(rA)/oligo(dT)15 as template by colometric streptavidin alkaline phosphate reporter assay | B | 6.01 | pIC50 | 980 | nM | IC50 | Eur J Med Chem (2012) 53: 229-234 [PMID:22575532] |
| 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 | 6.12 | pIC50 | 750 | nM | IC50 | Eur J Med Chem (2020) 185: 111874-111874 [PMID:31735575] |
| ChEMBL | Inhibition of wild-type HIV1 reverse transcriptase assessed as decrease in digoxigenin and biotin-dUTP incorporation in to DNA using poly(A)/oligo(dT)15 as template/primer after 1 hr by ELISA | B | 6.12 | pIC50 | 750 | nM | IC50 | Eur J Med Chem (2018) 151: 339-350 [PMID:29635166] |
| ChEMBL | Inhibition of RNA-dependent DNA polymerase activity of HIV1 subtype B reverse transcriptase M230L mutant by filter-based filtration assay | B | 6.16 | pIC50 | 696 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 2401-2408 [PMID:20308384] |
| ChEMBL | Inhibition of HIV1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation | B | 6.16 | pIC50 | 694.8 | nM | IC50 | Bioorg Med Chem (2022) 53: 116531-116531 [PMID:34890994] |
| ChEMBL | Inhibition of HIV1 reverse transcriptase assessed as incorporation of biotin-dUTP into poly(rA)-oligo(dT) | B | 6.26 | pIC50 | 550 | nM | IC50 | Eur J Med Chem (2012) 51: 60-66 [PMID:22405288] |
| ChEMBL | Inhibition of HIV 1 reverse transcriptase assessed as incorporation of biotin-dUTP into poly rA.dT by ELISA | B | 6.26 | pIC50 | 550 | nM | IC50 | Bioorg Med Chem (2013) 21: 2128-2134 [PMID:23415090] |
| ChEMBL | Inhibition of HIV-1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation into cDNA incubated for 1 hr with DIG-dUTP, biotin-dUTP and dTTP followed by transferring onto streptavidin-coated plate and measured after 1 hr by ELISA | B | 6.46 | pIC50 | 350 | nM | IC50 | Eur J Med Chem (2021) 211: 113063-113063 [PMID:33340914] |
| ChEMBL | Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase Y181C mutant by filter-based filtration assay | B | 6.59 | pIC50 | 257 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 4667-4672 [PMID:19704127] |
| ChEMBL | Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase G190A mutant by filter-based filtration assay | B | 6.72 | pIC50 | 191 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 4667-4672 [PMID:19704127] |
| ChEMBL | Inhibition of HIV1 reverse transcriptase assessed as inhibition of biotinylated dUTP incorporation after 1 hr by ELISA | B | 6.74 | pIC50 | 180 | nM | IC50 | Bioorg Med Chem (2014) 22: 1863-1872 [PMID:24581546] |
| 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 | 6.76 | pIC50 | 175 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 4667-4672 [PMID:19704127] |
| ChEMBL | Inhibition of wild type HIV1 reverse transcriptase Y181I mutant assessed as reduction in enzyme activity | B | 6.79 | pIC50 | 164 | nM | IC50 | J Med Chem (2014) 57: 9945-9957 [PMID:25418038] |
| ChEMBL | Inhibition of wild type HIV1 reverse transcriptase Y181I/Y181C mutant assessed as reduction in enzyme activity | B | 6.79 | pIC50 | 164 | 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 | 6.79 | pIC50 | 164 | 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 | 6.79 | pIC50 | 164 | nM | IC50 | J Med Chem (2017) 60: 6528-6547 [PMID:28628334] |
| 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 | 6.89 | pIC50 | 130 | nM | IC50 | Eur J Med Chem (2015) 93: 330-337 [PMID:25707013] |
| 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 | 6.89 | pIC50 | 129 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 4667-4672 [PMID:19704127] |
| ChEMBL | Inhibition of DNA-dependent DNA polymerase activity of wild type HIV1 subtype B reverse transcriptase by gel-based primer extension assay | B | 6.9 | pIC50 | 126 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 2401-2408 [PMID:20308384] |
| ChEMBL | Inhibition of HIV1 recombinant reverse transcriptase Y188L mutant by SPA heteropolymeric assay | B | 6.97 | pIC50 | 108 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 6020-6023 [PMID:20829038] |
| 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 | 6.97 | pIC50 | 107 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 4667-4672 [PMID:19704127] |
| ChEMBL | Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase DNA-dependent DNA polymerase activity by gel-based primer extension assay | B | 7.01 | pIC50 | 97 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 4667-4672 [PMID:19704127] |
| 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 | 7.05 | pIC50 | 90 | nM | IC50 | J Med Chem (2016) 59: 7991-8007 [PMID:27541578] |
| 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 | 7.05 | pIC50 | 89 | nM | IC50 | Eur J Med Chem (2015) 92: 754-765 [PMID:25626145] |
| 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 | 7.08 | pIC50 | 83 | nM | IC50 | Bioorg Med Chem (2014) 22: 2052-2059 [PMID:24631361] |
| ChEMBL | Inhibition of wild-type HIV1 reverse transcriptase assessed as incorporation of biotin-labeled dUTP | B | 7.15 | pIC50 | 71 | nM | IC50 | Bioorg Med Chem (2014) 22: 633-642 [PMID:24275349] |
| ChEMBL | Inhibition of RNA-dependent DNA polymerase activity of wild type HIV1 subtype B reverse transcriptase by filter-based filtration assay | B | 7.17 | pIC50 | 68 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 2401-2408 [PMID:20308384] |
| ChEMBL | Inhibition of wild type HIV-1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation in presence of template-primer incubated for 60 mins followed by transferring to streptavidin-coated plate and further incubation for 60 mins by ELISA | B | 7.23 | pIC50 | 59 | nM | IC50 | Bioorg Med Chem (2021) 40: 116195-116195 [PMID:33979774] |
| 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 | 7.3 | pIC50 | 50 | nM | IC50 | Bioorg Med Chem (2016) 24: 2476-2485 [PMID:27112451] |
| ChEMBL | Inhibition of HIV-1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation into cDNA measured after 1 hr by ELISA | B | 7.32 | pIC50 | 48 | nM | IC50 | Bioorg Med Chem (2021) 42: 116239-116239 [PMID:34090079] |
| ChEMBL | Inhibition of HIV1 RT Y188L mutant in presence of reconstituted template and viral nucleotides [digoxigenin (DIG)-dUTP, biotin-dUTP and dTTP] incubated for 1 hr by ELISA method | B | 7.34 | pIC50 | 46 | nM | IC50 | J Med Chem (2020) 63: 4837-4848 [PMID:32293182] |
| 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 | 7.4 | pIC50 | 40 | nM | IC50 | Eur J Med Chem (2021) 226: 113868-113868 [PMID:34583311] |
| ChEMBL | Inhibition of HIV1 RT E138K mutant in presence of reconstituted template and viral nucleotides [digoxigenin (DIG)-dUTP, biotin-dUTP and dTTP] incubated for 1 hr by ELISA method | B | 7.49 | pIC50 | 32 | nM | IC50 | J Med Chem (2020) 63: 4837-4848 [PMID:32293182] |
| ChEMBL | Inhibition of HIV1 reverse transcriptase p66/p51 V106A mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem (2016) 24: 2476-2485 [PMID:27112451] |
| ChEMBL | Inhibition of HIV1 reverse transcriptase p66/p51 Y181C mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem (2016) 24: 2476-2485 [PMID:27112451] |
| ChEMBL | Inhibition of HIV1 recombinant wild type reverse transcriptase by SPA heteropolymeric assay | B | 7.59 | pIC50 | 26 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 6020-6023 [PMID:20829038] |
| ChEMBL | Inhibition of HIV1 RT K103N mutant in presence of reconstituted template and viral nucleotides [digoxigenin (DIG)-dUTP, biotin-dUTP and dTTP] incubated for 1 hr by ELISA method | B | 7.6 | pIC50 | 25 | nM | IC50 | J Med Chem (2020) 63: 4837-4848 [PMID:32293182] |
| 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 | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2012) 55: 6634-6638 [PMID:22712652] |
| 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 | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2021) 226: 113868-113868 [PMID:34583311] |
| 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 | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2020) 208: 112696-112696 [PMID:32883642] |
| 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 | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem (2018) 26: 2051-2060 [PMID:29559197] |
| ChEMBL | Inhibition of wild type HIV1 reverse transcriptase K103N mutant assessed as reduction in enzyme activity | B | 7.7 | pIC50 | 20 | 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 | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2017) 60: 6528-6547 [PMID:28628334] |
| ChEMBL | Inhibition of HIV1 wild-type reverse transcriptase K103N mutant using [3H]dTTP by scintillation counting | B | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2014) 80: 101-111 [PMID:24769348] |
| 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 | 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 | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2021) 226: 113868-113868 [PMID:34583311] |
| ChEMBL | Inhibition of HIV1 RT K103N/Y181C mutant in presence of reconstituted template and viral nucleotides [digoxigenin (DIG)-dUTP, biotin-dUTP and dTTP] incubated for 1 hr by ELISA method | B | 7.72 | pIC50 | 19 | nM | IC50 | J Med Chem (2020) 63: 4837-4848 [PMID:32293182] |
| ChEMBL | Inhibition of HIV1 reverse transcriptase L100I/K103N double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay | B | 7.72 | pIC50 | 19 | nM | IC50 | Eur J Med Chem (2018) 158: 371-392 [PMID:30223123] |
| ChEMBL | Inhibition of HIV1 recombinant reverse transcriptase K103N/Y181C double mutant by SPA heteropolymeric assay | B | 7.72 | pIC50 | 19 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 6020-6023 [PMID:20829038] |
| 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 | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem (2016) 24: 3006-3022 [PMID:27234889] |
| ChEMBL | Inhibition of HIV1 RT Y181C mutant in presence of reconstituted template and viral nucleotides [digoxigenin (DIG)-dUTP, biotin-dUTP and dTTP] incubated for 1 hr by ELISA method | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (2020) 63: 4837-4848 [PMID:32293182] |
| ChEMBL | Inhibition of wild-type HIV-1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (2023) 66: 2102-2115 [PMID:36700940] |
| 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 | 7.77 | pIC50 | 17 | 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 | 7.77 | pIC50 | 17 | nM | IC50 | Bioorg Med Chem (2013) 21: 6477-6483 [PMID:24055077] |
| ChEMBL | Inhibition of wild-type HIV1 reverse transcriptase p66/p51 after 40 mins by spectrophotometry | B | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem (2014) 22: 2535-2541 [PMID:24680058] |
| ChEMBL | Inhibition of HIV-1 reverse transcriptase using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorometric analysis | B | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2022) 65: 8478-8492 [PMID:35649164] |
| ChEMBL | Inhibition of HIV1 RT L100I mutant in presence of reconstituted template and viral nucleotides [digoxigenin (DIG)-dUTP, biotin-dUTP and dTTP] incubated for 1 hr by ELISA method | B | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2020) 63: 4837-4848 [PMID:32293182] |
| ChEMBL | Inhibition of HIV1 RT in presence of reconstituted template and viral nucleotides [digoxigenin (DIG)-dUTP, biotin-dUTP and dTTP] incubated for 1 hr by ELISA method | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (2020) 63: 4837-4848 [PMID:32293182] |
| ChEMBL | Inhibition of wild type HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation into protein incubated for 1 hrs by ELISA | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (2021) 64: 13658-13675 [PMID:34432448] |
| ChEMBL | Inhibition of HIV1 wild-type reverse transcriptase L100I mutant using [3H]dTTP by scintillation counting | B | 7.92 | pIC50 | 12 | nM | IC50 | Eur J Med Chem (2014) 80: 101-111 [PMID:24769348] |
| ChEMBL | Inhibition of wild type HIV1 reverse transcriptase L100I mutant assessed as reduction in enzyme activity | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (2014) 57: 9945-9957 [PMID:25418038] |
| ChEMBL | Inhibition of wild type recombinant HIV-1 reverse transcriptase assessed as reduction of biotin-dUTP incorporation into protein using ABTS as substrate incubated for 1 hrs by ELISA analysis | B | 7.96 | pIC50 | 11 | nM | IC50 | Eur J Med Chem (2023) 247: 115045-115045 [PMID:36577216] |
| 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 | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2021) 64: 10297-10311 [PMID:34197708] |
| ChEMBL | Inhibition of recombinant wild type HIV1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation into template | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2021) 64: 4239-4256 [PMID:33734714] |
| 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 | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 3491-3495 [PMID:30318436] |
| 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 | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2023) 66: 8643-8665 [PMID:37255025] |
| ChEMBL | Inhibition of recombinant HIV-1 reverse transcriptase p66/p51 incubated for 40 mins by picogreen dye based spectrofluorometric assay | B | 7.96 | pIC50 | 11 | nM | IC50 | Eur J Med Chem (2019) 182: 111603-111603 [PMID:31421633] |
| ChEMBL | Inhibition of recombinant wild type HIV1 reverse transcriptase p66/p51 incubated for 40 mins by picogreen dye-based spectrofluorometric analysis | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2019) 62: 11430-11436 [PMID:31714780] |
| ChEMBL | Inhibition of recombinant HIV1 Reverse transcriptase p66/p51 using poly (rA)-oligo (dT) as template primer after 40 mins by spectrofluorometric analysis | B | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem (2015) 23: 6587-6593 [PMID:26385446] |
| 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 | 7.96 | pIC50 | 11 | nM | IC50 | ACS Med Chem Lett (2018) 9: 334-338 [PMID:29670696] |
| ChEMBL | Inhibition of wild type HIV1 p66/p51 reverse transcriptase using poly(rA) as template, oligo(dT)16 as primer and RNA/DNA as substrate measured after 40 mins by PICOGreen-dye based spectrofluorimetry analysis | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2021) 64: 13604-13621 [PMID:34496571] |
| 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 | 7.96 | pIC50 | 11 | nM | IC50 | Eur J Med Chem (2016) 121: 352-363 [PMID:27267005] |
| ChEMBL | Inhibition of HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation into template incubated for 1 hr by ELISA | B | 7.96 | pIC50 | 11 | nM | IC50 | Eur J Med Chem (2021) 213: 113051-113051 [PMID:33279288] |
| ChEMBL | Inhibition of wild-type HIV1 Reverse transcriptase p66/p51 assessed as relative fluorescence signal after 40 mins | B | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem (2015) 23: 3860-3868 [PMID:25907370] |
| ChEMBL | Inhibition of recombinant wild type p66/p51 HIV1 reverse transcriptase incubated for 40 mins by picogreen dye-based spectrofluorometric analysis | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2022) 65: 2122-2138 [PMID:35073089] |
| ChEMBL | Inhibition of recombinant wild type p66/p51 HIV1 reverse transcriptase incubated for 40 mins by picogreen dye-based spectrofluorometric analysis | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2021) 64: 5067-5081 [PMID:33851529] |
| ChEMBL | Inhibition of recombinant HIV1 reverse transcriptase using (DIG)-dUTP and biotin-labeled dNTPs as substrate after 1 hr by ELISA | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2019) 62: 1484-1501 [PMID:30624934] |
| 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 | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2019) 62: 2083-2098 [PMID:30721060] |
| ChEMBL | Inhibition of recombinant wild type HIV-1 reverse transcriptase using DNA/RNA as substrate incubated for 40 mins by Pico-green dye based spectrofluorometric analysis | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2023) 66: 4755-4767 [PMID:36996328] |
| ChEMBL | Inhibition of HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation into template incubated for 1 hr by ELISA | B | 7.96 | pIC50 | 10.96 | nM | IC50 | Eur J Med Chem (2021) 213: 113051-113051 [PMID:33279288] |
| 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 | 7.96 | pIC50 | 10.96 | nM | IC50 | J Med Chem (2019) 62: 2083-2098 [PMID:30721060] |
| 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 | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2012) 55: 6634-6638 [PMID:22712652] |
| ChEMBL | Inhibition of wild type HIV1 reverse transcriptase V106A mutant assessed as reduction in enzyme activity | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2014) 57: 9945-9957 [PMID:25418038] |
| ChEMBL | Inhibition of HIV1 wild type reverse transcriptase p66/p51 using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem (2016) 24: 2476-2485 [PMID:27112451] |
| ChEMBL | Inhibition of HIV1 reverse transcriptase p66/p51 L100I mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem (2016) 24: 2476-2485 [PMID:27112451] |
| ChEMBL | Inhibition of HIV1 reverse transcriptase p66/p51 K103N mutant 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 wild type HIV1 reverse transcriptase assessed as reduction in enzyme activity | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2014) 57: 9945-9957 [PMID:25418038] |
| ChEMBL | Inhibition of HIV1 wild-type reverse transcriptase using [3H]dTTP by scintillation counting | B | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2014) 80: 101-111 [PMID:24769348] |
| 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 | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2017) 60: 6528-6547 [PMID:28628334] |
| ChEMBL | Inhibition of HIV1 wild-type reverse transcriptase V106A mutant using [3H]dTTP by scintillation counting | B | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2014) 80: 101-111 [PMID:24769348] |
| 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 | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2017) 140: 383-391 [PMID:28987601] |
| 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 | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2020) 208: 112696-112696 [PMID:32883642] |
| 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 | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2012) 55: 6634-6638 [PMID:22712652] |
| 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 | 8 | pIC50 | 10 | 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 | 8 | pIC50 | 10 | 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 | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2021) 226: 113868-113868 [PMID:34583311] |
| ChEMBL | Inhibition of wild type recombinant HIV-1 reverse transcriptase using biotin-labelled dNTPs as substrate assessed as inhibition of biotin-labelled UTP incorporation incubated for 1 hr by ELISA | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2022) 65: 15608-15626 [PMID:36411036] |
| ChEMBL | Inhibition of HIV-1 reverse transcriptase incubated for 1 hrs in presence of biotin-labeled dNTPs by ELISA assay | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem (2023) 96: 117484-117484 [PMID:37976805] |
| ChEMBL | Inhibition of HIV1 RT V106A/F227L mutant in presence of reconstituted template and viral nucleotides [digoxigenin (DIG)-dUTP, biotin-dUTP and dTTP] incubated for 1 hr by ELISA method | B | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2020) 63: 4837-4848 [PMID:32293182] |
| 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 | 8.1 | pIC50 | 8 | nM | IC50 | Eur J Med Chem (2023) 246: 114957-114957 [PMID:36446205] |
| ChEMBL | Inhibition of HIV1 reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay | B | 8.15 | pIC50 | 7 | nM | IC50 | Eur J Med Chem (2018) 158: 371-392 [PMID:30223123] |
| ChEMBL | Inhibition of HIV1 reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay | B | 8.34 | pIC50 | 4.6 | nM | IC50 | Eur J Med Chem (2018) 158: 371-392 [PMID:30223123] |
| ChEMBL | Inhibition of HIV1 reverse transcriptase K103N/Y188C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay | B | 8.37 | pIC50 | 4.3 | nM | IC50 | Eur J Med Chem (2018) 158: 371-392 [PMID:30223123] |
| ChEMBL | Inhibition of HIV1 reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay | B | 8.48 | pIC50 | 3.3 | nM | IC50 | Eur J Med Chem (2018) 158: 371-392 [PMID:30223123] |
| ChEMBL | Inhibition of HIV1 isolate R8 reverse transcriptase Y181C mutant after 90 mins by electrochemiluminescence analysis | B | 8.71 | pIC50 | 1.96 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 2424-2431 [PMID:19289522] |
| ChEMBL | Inhibition of HIV1 LAI reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay | B | 8.85 | pIC50 | 1.4 | nM | IC50 | Eur J Med Chem (2018) 158: 371-392 [PMID:30223123] |
| ChEMBL | Inhibition of HIV1 isolate R8 reverse transcriptase K103N mutant after 90 mins by electrochemiluminescence analysis | B | 8.89 | pIC50 | 1.3 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 2424-2431 [PMID:19289522] |
| ChEMBL | Inhibition of HIV1 reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay | B | 8.92 | pIC50 | 1.2 | nM | IC50 | Eur J Med Chem (2018) 158: 371-392 [PMID:30223123] |
| ChEMBL | Inhibition of HIV1 isolate R8 reverse transcriptase after 90 mins | B | 9.22 | pIC50 | 0.6 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 2424-2431 [PMID:19289522] |
| 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 | 7.34 | pEC50 | 46 | 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 by MTT assay | B | 7.46 | pEC50 | 34.4 | 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 | 7.53 | pEC50 | 29.4 | nM | EC50 | J Med Chem (2017) 60: 4424-4443 [PMID:28481112] |
| ChEMBL | Inhibition of reverse transcriptase F227L/V106A double mutant in HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | B | 7.6 | pEC50 | 25 | nM | EC50 | Eur J Med Chem (2021) 214: 113204-113204 [PMID:33567378] |
| 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 | 7.69 | pEC50 | 20.5 | 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 | 7.72 | pEC50 | 18.9 | nM | EC50 | J Med Chem (2021) 64: 5067-5081 [PMID:33851529] |
| 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 | 7.74 | pEC50 | 18.4 | nM | EC50 | Eur J Med Chem (2020) 202: 112549-112549 [PMID:32712537] |
| 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 | 7.74 | pEC50 | 18 | nM | EC50 | Eur J Med Chem (2021) 214: 113204-113204 [PMID:33567378] |
| 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 | 7.77 | pEC50 | 17 | 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 | 7.77 | pEC50 | 17 | 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 | 7.79 | pEC50 | 16.3 | nM | EC50 | Eur J Med Chem (2020) 202: 112549-112549 [PMID:32712537] |
| 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 | 7.8 | pEC50 | 15.7 | nM | EC50 | J Med Chem (2017) 60: 4424-4443 [PMID:28481112] |
| 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 | 7.84 | pEC50 | 14.4 | nM | EC50 | J Med Chem (2017) 60: 4424-4443 [PMID:28481112] |
| 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 | 7.91 | pEC50 | 12.2 | nM | EC50 | Eur J Med Chem (2020) 202: 112549-112549 [PMID:32712537] |
| 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 | 7.92 | pEC50 | 12 | nM | EC50 | Eur J Med Chem (2016) 122: 185-195 [PMID:27371922] |
| ChEMBL | Inhibition of HIV-1 p66/p51 reverse transcriptase L100I mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis | B | 7.97 | pEC50 | 10.7 | nM | EC50 | J Med Chem (2021) 64: 5067-5081 [PMID:33851529] |
| 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 | 8.04 | pEC50 | 9.2 | 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 | 8.05 | pEC50 | 9 | nM | EC50 | Eur J Med Chem (2021) 214: 113204-113204 [PMID:33567378] |
| 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 | 8.1 | pEC50 | 8 | nM | EC50 | Eur J Med Chem (2021) 214: 113204-113204 [PMID:33567378] |
| ChEMBL | Inhibition of HIV1 reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity by MTT assay | B | 8.27 | pEC50 | 5.39 | nM | EC50 | ACS Med Chem Lett (2018) 9: 370-375 [PMID:29670703] |
| 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 | 8.27 | pEC50 | 5.38 | nM | EC50 | J Med Chem (2017) 60: 4424-4443 [PMID:28481112] |
| ChEMBL | Inhibition of HIV RT K103N/Y181C mutant by cell based assay | B | 8.3 | pEC50 | 5 | nM | EC50 | Eur J Med Chem (2013) 65: 134-143 [PMID:23707918] |
| 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 | 8.4 | pEC50 | 4 | nM | EC50 | ACS Med Chem Lett (2018) 9: 370-375 [PMID:29670703] |
| ChEMBL | Inhibition of wild-type HIV-1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation | B | 8.45 | pEC50 | 3.55 | nM | EC50 | J Med Chem (2023) 66: 2102-2115 [PMID:36700940] |
| ChEMBL | Inhibition of HIV-1 p66/p51 reverse transcriptase K103N mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis | B | 8.47 | pEC50 | 3.4 | 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 | 8.52 | pEC50 | 3 | 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 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 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 | 8.63 | pEC50 | 2.35 | nM | EC50 | J Med Chem (2017) 60: 4424-4443 [PMID:28481112] |
| ChEMBL | Inhibition of reverse transcriptase K103N mutant in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | B | 8.64 | pEC50 | 2.3 | nM | EC50 | Eur J Med Chem (2020) 202: 112549-112549 [PMID:32712537] |
| 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 | 8.7 | pEC50 | 2 | nM | EC50 | Eur J Med Chem (2016) 122: 185-195 [PMID:27371922] |
| ABCC1/Multidrug resistance-associated protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3004] [GtoPdb: 779] [UniProtKB: P33527] | ||||||||
| ChEMBL | Inhibition of MRP1 expressed in MDCK2 cells assessed as cell growth inhibition by calcein and pheophorbide A efflux assays | B | 5.07 | pIC50 | 8500 | nM | IC50 | Antimicrob Agents Chemother (2011) 55: 1282-1284 [PMID:21189339] |
| ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] | ||||||||
| ChEMBL | Inhibition of MDR1 expressed in MDCK2 cells assessed as inhibition of cell proliferation by calcein and pheophorbide A efflux assays | B | 5.12 | pIC50 | 7600 | nM | IC50 | Antimicrob Agents Chemother (2011) 55: 1282-1284 [PMID:21189339] |
| 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 | Antimalarial activity against Plasmodium falciparum W2mef trophozoite form by hoechst 33342-thiazole orange stain based flow cytometry assay | F | 6.14 | pIC50 | 726 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5452-5457 [PMID:19666223] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum W2mef schizont form by hoechst 33342-thiazole orange stain based flow cytometry assay | F | 6.15 | pIC50 | 716 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5452-5457 [PMID:19666223] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum W2mef assessed as DNA positive erythrocytes by hoechst 33342-thiazole orange stain based flow cytometry assay | F | 6.3 | pIC50 | 506 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5452-5457 [PMID:19666223] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum W2mef ring form by hoechst 33342-thiazole orange stain based flow cytometry assay | F | 6.39 | pIC50 | 409 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5452-5457 [PMID:19666223] |
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]
