| Assay ID | Title | Year | Journal | Article |
|---|
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1722856 | Antiproliferative activity against human HeLa cells assessed as reduction in cell viability at 0.1 to 10 uM supplemented with fresh medium containing compound every other day for 6 days by CellTiter-Glo assay | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
| Discovery of First-in-Class Protein Arginine Methyltransferase 5 (PRMT5) Degraders. |
| AID1911355 | Inhibition of PRMT5 (unknown origin) by biochemical assay | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
| Structure-Aided Design, Synthesis, and Biological Evaluation of Potent and Selective Non-Nucleoside Inhibitors Targeting Protein Arginine Methyltransferase 5. |
| AID1530687 | Induction of apoptosis in human KARPAS422 cells assessed as apoptotic cells at 2 uM after 48 hrs by AnnexinV-FITC staining-based flow cytometric analysis (Rvb = 1.6%) | 2018 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
| Discovery of new potent protein arginine methyltransferase 5 (PRMT5) inhibitors by assembly of key pharmacophores from known inhibitors. |
| AID1530690 | Induction of apoptosis in human KARPAS422 cells assessed as apoptotic cells at 16 uM after 48 hrs by AnnexinV-FITC staining-based flow cytometric analysis (Rvb = 1.6%) | 2018 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
| Discovery of new potent protein arginine methyltransferase 5 (PRMT5) inhibitors by assembly of key pharmacophores from known inhibitors. |
| AID1530689 | Induction of apoptosis in human KARPAS422 cells assessed as viable cells at 16 uM after 48 hrs by AnnexinV-FITC staining-based flow cytometric analysis (Rvb = 86.6%) | 2018 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
| Discovery of new potent protein arginine methyltransferase 5 (PRMT5) inhibitors by assembly of key pharmacophores from known inhibitors. |
| AID1825239 | Inhibition of MTA-bound human PRMT5 co-complexed with MEP50 using biotin labelled histone H4 peptide (1 to 15) as substrate assessed as inhibition of tritiated methyl group transfer from SAM to histone H4 preincubated for 20 mins followed by SAM addition | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of |
| AID1722858 | Antiproliferative activity against human A172 cells assessed as reduction in cell viability at 0.1 to 10 uM supplemented with fresh medium containing compound every other day for 6 days by CellTiter-Glo assay | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
| Discovery of First-in-Class Protein Arginine Methyltransferase 5 (PRMT5) Degraders. |
| AID1768581 | Displacement of fluorophore-labeled RIOK1 from human PRMT5/WDR77 hetero octameric complex expressed in Sf9 cells by competition fluorescence polarization (FP) assay | 2021 | Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
| Discovery of a First-in-Class Inhibitor of the PRMT5-Substrate Adaptor Interaction. |
| AID1530682 | Cell cycle arrest in human KARPAS422 cells assessed as accumulation of cells at G2/M phase at 2 uM after 48 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 12.22%) | 2018 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
| Discovery of new potent protein arginine methyltransferase 5 (PRMT5) inhibitors by assembly of key pharmacophores from known inhibitors. |
| AID1825279 | Binding affinity to MTA-bound human PRMT5 assessed as dissociation constant by SPR assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of |
| AID1530650 | Antiproliferative activity against human MV4-11 cells after 4 days by cell titer-glo luminescent cell viability assay | 2018 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
| Discovery of new potent protein arginine methyltransferase 5 (PRMT5) inhibitors by assembly of key pharmacophores from known inhibitors. |
| AID1722857 | Antiproliferative activity against human A549 cells assessed as reduction in cell viability at 0.1 to 10 uM supplemented with fresh medium containing compound every other day for 6 days by CellTiter-Glo assay | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
| Discovery of First-in-Class Protein Arginine Methyltransferase 5 (PRMT5) Degraders. |
| AID1613956 | Inhibition of recombinant human N-terminal FLAG-tagged PRMT5 (2 to end residues)/human N-terminal His-tagged MEP50 (2 to end residues) expressed in HEK293F cells using H4 peptide as substrate preincubated for 15 mins followed by substrate and [3H]SAM addi | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Discovery of 2-substituted-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-1,2,3,4-tetrahydroisoquinoline-6-carboxamide as potent and selective protein arginine methyltransferases 5 inhibitors: Design, synthesis and biological evaluation. |
| AID1530685 | Cell cycle arrest in human KARPAS422 cells assessed as accumulation of cells at G2/M phase at 16 uM after 48 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 12.22%) | 2018 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
| Discovery of new potent protein arginine methyltransferase 5 (PRMT5) inhibitors by assembly of key pharmacophores from known inhibitors. |
| AID1722859 | Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability at 0.1 to 10 uM supplemented with fresh medium containing compound every other day for 6 days by CellTiter-Glo assay | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
| Discovery of First-in-Class Protein Arginine Methyltransferase 5 (PRMT5) Degraders. |
| AID1530645 | Inhibition of human recombinant PRMT5/MEP50 expressed in 293-F cells using histone 4 peptide as substrate after 90 mins in presence of [3H]SAM by autoradiographic analysis | 2018 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
| Discovery of new potent protein arginine methyltransferase 5 (PRMT5) inhibitors by assembly of key pharmacophores from known inhibitors. |
| AID1722836 | Inhibition of human PRMT5/MEP50 assessed as reduction in methyltransferase activity using histone 4 peptide as substrate in presence of [3H]SAM incubated for 30 mins | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
| Discovery of First-in-Class Protein Arginine Methyltransferase 5 (PRMT5) Degraders. |
| AID1722831 | Induction of VHL-mediated PRMT5 degradation in human MCF7 cells assessed as reduction in SDMA level incubated for 6 days by Western blot analysis | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
| Discovery of First-in-Class Protein Arginine Methyltransferase 5 (PRMT5) Degraders. |
| AID1530652 | Antiproliferative activity against human SU-DHL4 cells after 4 days by cell titer-glo luminescent cell viability assay | 2018 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
| Discovery of new potent protein arginine methyltransferase 5 (PRMT5) inhibitors by assembly of key pharmacophores from known inhibitors. |
| AID1685694 | Time during which unbound drug concentration exceeds IC90 for inhibition of PRMT5 in human Z138 cells in CD-1 mouse at 100 mg/kg, po | 2016 | ACS medicinal chemistry letters, Feb-11, Volume: 7, Issue:2
| Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666. |
| AID1530653 | Antiproliferative activity against human KARPAS422 cells after 4 days by cell titer-glo luminescent cell viability assay | 2018 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
| Discovery of new potent protein arginine methyltransferase 5 (PRMT5) inhibitors by assembly of key pharmacophores from known inhibitors. |
| AID1530670 | Cell cycle arrest in human KARPAS422 cells assessed as accumulation of cells at G1 phase at 2 uM after 48 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 41.35%) | 2018 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
| Discovery of new potent protein arginine methyltransferase 5 (PRMT5) inhibitors by assembly of key pharmacophores from known inhibitors. |
| AID1722833 | Induction of VHL-mediated PRMT5 degradation in human MCF7 cells at 5 uM incubated for 6 days by Western blot analysis | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
| Discovery of First-in-Class Protein Arginine Methyltransferase 5 (PRMT5) Degraders. |
| AID1530683 | Cell cycle arrest in human KARPAS422 cells assessed as accumulation of cells at G1 phase at 16 uM after 48 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 41.35%) | 2018 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
| Discovery of new potent protein arginine methyltransferase 5 (PRMT5) inhibitors by assembly of key pharmacophores from known inhibitors. |
| AID1685690 | Inhibition of human full length FLAG-tagged PRMT5/human His6-tagged MEP50 expressed in baculovirus-infected Sf9 cells assessed as reduction in tritium incorporation into peptide substrate using human Histone H4 (1 to 15 residues) and [3H]SAM as substrate | 2016 | ACS medicinal chemistry letters, Feb-11, Volume: 7, Issue:2
| Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666. |
| AID1396189 | Antiproliferative activity against human Z138 cells measured after 12 days post culturing by guava via count reagent assay | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Protein Arginine Methyltransferase 5 (PRMT5) as an Anticancer Target and Its Inhibitor Discovery. |
| AID1396190 | Antiproliferative activity against human Maver1 cells measured after 12 days post culturing by guava via count reagent assay | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Protein Arginine Methyltransferase 5 (PRMT5) as an Anticancer Target and Its Inhibitor Discovery. |
| AID1396186 | Oral bioavailability in mouse at 10 mg/kg | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Protein Arginine Methyltransferase 5 (PRMT5) as an Anticancer Target and Its Inhibitor Discovery. |
| AID1445895 | Uncompetitive inhibition of recombinant human N-terminal FLAG-tagged PRMT5 (2 to end residues) /human N-terminal His-tagged MEP50 (2 to end residues) expressed in HEK293F cells using peptide substrate preincubated for 15 mins followed by substrate/[3H]-SA | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
| Potent, Selective, and Cell Active Protein Arginine Methyltransferase 5 (PRMT5) Inhibitor Developed by Structure-Based Virtual Screening and Hit Optimization. |
| AID1396191 | Inhibition of PRMT5 (unknown origin) using H4R3 as substrate by HTRF assay | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Protein Arginine Methyltransferase 5 (PRMT5) as an Anticancer Target and Its Inhibitor Discovery. |
| AID1530651 | Antiproliferative activity against human Pfeiffer cells after 4 days by cell titer-glo luminescent cell viability assay | 2018 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
| Discovery of new potent protein arginine methyltransferase 5 (PRMT5) inhibitors by assembly of key pharmacophores from known inhibitors. |
| AID1685691 | Inhibition of PRMT5 in human Z138 cells assessed as reduction in symmetrical dimethylation of arginine containing substrate using SmD3 as substrate incubated for 4 days by In-cell western assay | 2016 | ACS medicinal chemistry letters, Feb-11, Volume: 7, Issue:2
| Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666. |
| AID1685692 | Antiproliferative activity against human Z138 cells incubated for 5 days by cell titer-glo assay | 2016 | ACS medicinal chemistry letters, Feb-11, Volume: 7, Issue:2
| Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666. |
| AID1685693 | Protein binding in CD-1 mouse plasma | 2016 | ACS medicinal chemistry letters, Feb-11, Volume: 7, Issue:2
| Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666. |
| AID1768583 | Stability in human plasma assessed as compound remaining relative to control | 2021 | Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
| Discovery of a First-in-Class Inhibitor of the PRMT5-Substrate Adaptor Interaction. |
| AID1530646 | Inhibition of recombinant human N-terminal FLAG-tagged PRMT5 (2 to end residues) /human N-terminal His-tagged MEP50 (2 to end residues) expressed in HEK293F cells pretreated for 15 mins followed by substrate and [3H]-SAM addition measured after 60 mins by | 2018 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
| Discovery of new potent protein arginine methyltransferase 5 (PRMT5) inhibitors by assembly of key pharmacophores from known inhibitors. |
| AID1530688 | Induction of apoptosis in human KARPAS422 cells assessed as apoptotic cells at necrotic cells at 2 uM after 48 hrs by AnnexinV-FITC staining-based flow cytometric analysis (Rvb = 2.8%) | 2018 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
| Discovery of new potent protein arginine methyltransferase 5 (PRMT5) inhibitors by assembly of key pharmacophores from known inhibitors. |
| AID1530691 | Induction of apoptosis in human KARPAS422 cells assessed as apoptotic cells at necrotic cells at 16 uM after 48 hrs by AnnexinV-FITC staining-based flow cytometric analysis (Rvb = 2.8%) | 2018 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
| Discovery of new potent protein arginine methyltransferase 5 (PRMT5) inhibitors by assembly of key pharmacophores from known inhibitors. |
| AID1396192 | Antitumor activity against human Z138 cells xenografted in SCID mouse assessed as tumor growth inhibition at 200 mg/kg, po BID administered for 21 days | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Protein Arginine Methyltransferase 5 (PRMT5) as an Anticancer Target and Its Inhibitor Discovery. |
| AID1445894 | Competitive inhibition of recombinant human N-terminal FLAG-tagged PRMT5 (2 to end residues) /human N-terminal His-tagged MEP50 (2 to end residues) expressed in HEK293F cells using peptide substrate preincubated for 15 mins followed by substrate/[3H]-SAM | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
| Potent, Selective, and Cell Active Protein Arginine Methyltransferase 5 (PRMT5) Inhibitor Developed by Structure-Based Virtual Screening and Hit Optimization. |
| AID1530681 | Cell cycle arrest in human KARPAS422 cells assessed as accumulation of cells at S phase at 2 uM after 48 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 46.43%) | 2018 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
| Discovery of new potent protein arginine methyltransferase 5 (PRMT5) inhibitors by assembly of key pharmacophores from known inhibitors. |
| AID1396193 | Antitumor activity against human Maver1 cells xenografted in SCID mouse assessed as tumor growth inhibition at 200 mg/kg, po BID administered for 21 days | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Protein Arginine Methyltransferase 5 (PRMT5) as an Anticancer Target and Its Inhibitor Discovery. |
| AID1396188 | Plasma clearance in mouse at 2 mg/kg, iv | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Protein Arginine Methyltransferase 5 (PRMT5) as an Anticancer Target and Its Inhibitor Discovery. |
| AID1825238 | Inhibition of human PRMT5 co-complexed with MEP50 in absence of MTA using biotin labelled histone H4 peptide (1 to15) as substrate assessed as inhibition of tritiated methyl group transfer from SAM to histone H4 preincubated for 20 mins followed by SAM ad | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of |
| AID1911326 | Inhibition of PRMT5 in human A-375 cells assessed as decrease in sMDA levels measured after 48 hrs by Western blot analysis | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
| Structure-Aided Design, Synthesis, and Biological Evaluation of Potent and Selective Non-Nucleoside Inhibitors Targeting Protein Arginine Methyltransferase 5. |
| AID1768584 | Stability in mouse plasma assessed as compound remaining relative to control | 2021 | Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
| Discovery of a First-in-Class Inhibitor of the PRMT5-Substrate Adaptor Interaction. |
| AID1530686 | Induction of apoptosis in human KARPAS422 cells assessed as viable cells at 2 uM after 48 hrs by AnnexinV-FITC staining-based flow cytometric analysis (Rvb = 86.6%) | 2018 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
| Discovery of new potent protein arginine methyltransferase 5 (PRMT5) inhibitors by assembly of key pharmacophores from known inhibitors. |
| AID1530684 | Cell cycle arrest in human KARPAS422 cells assessed as accumulation of cells at S phase at 16 uM after 48 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 46.43%) | 2018 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
| Discovery of new potent protein arginine methyltransferase 5 (PRMT5) inhibitors by assembly of key pharmacophores from known inhibitors. |
| AID1494598 | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [3H]-SAM by Topcount method | 2018 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9
| Identification of a novel selective small-molecule inhibitor of protein arginine methyltransferase 5 (PRMT5) by virtual screening, resynthesis and biological evaluations. |
| AID1613958 | Antiproliferative activity against human MV4-11 cells supplemented with fresh medium containing compound every 4 days measured on day 12 by Celltiter-glo luminescent cell viability assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Discovery of 2-substituted-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-1,2,3,4-tetrahydroisoquinoline-6-carboxamide as potent and selective protein arginine methyltransferases 5 inhibitors: Design, synthesis and biological evaluation. |
| AID1530654 | Inhibition of PRMT5 in human KARPAS422 cells assessed as decrease in symmetric arginine dimethylation of SmD3 after 4 days by Western blot analysis | 2018 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
| Discovery of new potent protein arginine methyltransferase 5 (PRMT5) inhibitors by assembly of key pharmacophores from known inhibitors. |
| AID1396187 | Volume of distribution in mouse at 2 mg/kg, iv | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Protein Arginine Methyltransferase 5 (PRMT5) as an Anticancer Target and Its Inhibitor Discovery. |
| AID1613957 | Antiproliferative activity against human MV4-11 cells supplemented with fresh medium containing compound every 4 days measured on day 8 by Celltiter-glo luminescent cell viability assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Discovery of 2-substituted-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-1,2,3,4-tetrahydroisoquinoline-6-carboxamide as potent and selective protein arginine methyltransferases 5 inhibitors: Design, synthesis and biological evaluation. |
| AID1768582 | Solubility in PBS buffer | 2021 | Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
| Discovery of a First-in-Class Inhibitor of the PRMT5-Substrate Adaptor Interaction. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |