| Assay ID | Title | Year | Journal | Article |
|---|
| 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. |
| 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. |
| AID1434445 | Drug metabolism in human liver microsomes assessed as P+GSH-2 adduct formation at 20 uM in presence of GSH measured after 1 hr by UPLC-MS/MS method | 2017 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
| Mitigation of reactive metabolite formation for a series of 3-amino-2-pyridone inhibitors of Bruton's tyrosine kinase (BTK). |
| AID1176493 | Clearance in Sprague-Dawley rat at 2 mg/kg, po measured during 2 mins to 24 hrs period post dose by LC/MS/MS method | 2015 | Bioorganic & medicinal chemistry, Jan-15, Volume: 23, Issue:2
| Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton's tyrosine kinase inhibitors. |
| AID1357747 | Inhibition of BTK (unknown origin) | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review. |
| AID1763498 | Inhibition of human YES1 | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Discovery of potent and selective reversible Bruton's tyrosine kinase inhibitors. |
| AID1763454 | Efflux ratio of apparent permeability in human Caco-2 cells | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Discovery of potent and selective reversible Bruton's tyrosine kinase inhibitors. |
| AID1176498 | Oral bioavailability in Sprague-Dawley rat at 2 mg/kg measured during 2 mins to 24 hrs period post dose by LC/MS/MS method | 2015 | Bioorganic & medicinal chemistry, Jan-15, Volume: 23, Issue:2
| Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton's tyrosine kinase inhibitors. |
| AID1763451 | Inhibition of BTK in human whole blood | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Discovery of potent and selective reversible Bruton's tyrosine kinase inhibitors. |
| AID671883 | Inhibition of hypersensitive immune responses in rat passive cutaneous anaphylaxis model at 30 mg/kg | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies. |
| AID1357748 | Inhibition of TEC (unknown origin) | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review. |
| AID1763452 | Inhibition of BTK in human PBMC | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Discovery of potent and selective reversible Bruton's tyrosine kinase inhibitors. |
| AID1176490 | Apparent volume of distribution in Sprague-Dawley rat at 1 mg/kg, iv measured during 2 mins to 24 hrs period post dose by LC/MS/MS method | 2015 | Bioorganic & medicinal chemistry, Jan-15, Volume: 23, Issue:2
| Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton's tyrosine kinase inhibitors. |
| AID1763492 | Inhibition of human FGR | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Discovery of potent and selective reversible Bruton's tyrosine kinase inhibitors. |
| AID1176496 | Half life in Sprague-Dawley rat at 1 mg/kg, iv measured during 2 mins to 24 hrs period post dose by LC/MS/MS method | 2015 | Bioorganic & medicinal chemistry, Jan-15, Volume: 23, Issue:2
| Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton's tyrosine kinase inhibitors. |
| AID1357756 | Inhibition of BTK (unknown origin) assessed as reduction in TNF production | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review. |
| AID1176484 | Inhibition of collagen-induced arthritis in Wistar rat assessed as reduction in disease progression at 20 mg/kg, po dosed for 13 days starting from day 14 post collagen challenge | 2015 | Bioorganic & medicinal chemistry, Jan-15, Volume: 23, Issue:2
| Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton's tyrosine kinase inhibitors. |
| AID1176492 | Clearance in Sprague-Dawley rat at 1 mg/kg, iv measured during 2 mins to 24 hrs period post dose by LC/MS/MS method | 2015 | Bioorganic & medicinal chemistry, Jan-15, Volume: 23, Issue:2
| Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton's tyrosine kinase inhibitors. |
| AID671880 | Selectivity index, ratio of inhibition of SLK to IC50 for BTK | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies. |
| AID1433167 | Inhibition of BTK in human Ramos cells assessed as inhibition of anti human IgM-induced calcium influx preincubated for 20 mins in dark followed by anti human IgM induction for 8 mins by FLIPR assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
| Pyrrolo[2,3-b]pyridine derivatives as potent Bruton's tyrosine kinase inhibitors. |
| AID1763455 | Inhibition of human ERG at 10 uM | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Discovery of potent and selective reversible Bruton's tyrosine kinase inhibitors. |
| AID1434446 | Drug metabolism in human liver microsomes assessed as P+GSH+O-2 adduct formation at 20 uM in presence of GSH measured after 1 hr by UPLC-MS/MS method | 2017 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
| Mitigation of reactive metabolite formation for a series of 3-amino-2-pyridone inhibitors of Bruton's tyrosine kinase (BTK). |
| AID1433166 | Inhibition of recombinant human His-tagged full length BTK expressed in baculovirus using biotin labeled peptide substrate after 1 hr by HRTF kinase/TR-FRET assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
| Pyrrolo[2,3-b]pyridine derivatives as potent Bruton's tyrosine kinase inhibitors. |
| AID1433170 | AUClast in Sprague-Dawley rat at 4 mg/kg, po by LC/MS/MS analysis | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
| Pyrrolo[2,3-b]pyridine derivatives as potent Bruton's tyrosine kinase inhibitors. |
| AID671739 | Inhibition of IgM-stimulated CD69 expression in human whole blood | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies. |
| AID671875 | Inhibition of immobilized immune complex-stimulated TNFalpha production in macrophages | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies. |
| AID1763488 | Solubility of the compound in FaSSIF | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Discovery of potent and selective reversible Bruton's tyrosine kinase inhibitors. |
| AID1192610 | Inhibition of BTK (unknown origin) after 1 hr by TR-FRET analysis | 2015 | Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4
| Discovery of novel Bruton's tyrosine kinase (BTK) inhibitors bearing a pyrrolo[2,3-d]pyrimidine scaffold. |
| AID1176495 | Mean residence time (0 to t) in Sprague-Dawley rat at 2 mg/kg, po measured during 2 mins to 24 hrs period post dose by LC/MS/MS method | 2015 | Bioorganic & medicinal chemistry, Jan-15, Volume: 23, Issue:2
| Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton's tyrosine kinase inhibitors. |
| AID1176486 | Cmax in Sprague-Dawley rat at 1 mg/kg, iv measured during 2 mins to 24 hrs period post dose by LC/MS/MS method | 2015 | Bioorganic & medicinal chemistry, Jan-15, Volume: 23, Issue:2
| Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton's tyrosine kinase inhibitors. |
| AID1763497 | Inhibition of human TEC | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Discovery of potent and selective reversible Bruton's tyrosine kinase inhibitors. |
| AID671881 | Inhibition of IgE-Fce cross-linking induced histamine release in mast cells | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies. |
| AID1192611 | Inhibition of BTK in human Ramos cells after 20 mins by fluorescence assay | 2015 | Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4
| Discovery of novel Bruton's tyrosine kinase (BTK) inhibitors bearing a pyrrolo[2,3-d]pyrimidine scaffold. |
| AID1434441 | Drug metabolism in human liver microsomes assessed as covalent binding per mg protein at 10 uM preincubated for 5 mins followed by NADPH addition measured after 30 mins by liquid scintillation counting | 2017 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
| Mitigation of reactive metabolite formation for a series of 3-amino-2-pyridone inhibitors of Bruton's tyrosine kinase (BTK). |
| AID1763491 | Inhibition of human BTK | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Discovery of potent and selective reversible Bruton's tyrosine kinase inhibitors. |
| AID1433169 | Tmax in Sprague-Dawley rat at 4 mg/kg, po by LC/MS/MS analysis | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
| Pyrrolo[2,3-b]pyridine derivatives as potent Bruton's tyrosine kinase inhibitors. |
| AID1763496 | Inhibition of human BMX | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Discovery of potent and selective reversible Bruton's tyrosine kinase inhibitors. |
| AID1763453 | Apparent permeability of the compound across apical to basolateral side in human Caco-2 cells | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Discovery of potent and selective reversible Bruton's tyrosine kinase inhibitors. |
| AID1357752 | Inhibition of SLK (unknown origin) | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review. |
| AID1763450 | Inhibition of BTK (unknown origin) | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Discovery of potent and selective reversible Bruton's tyrosine kinase inhibitors. |
| AID1176488 | AUC in Sprague-Dawley rat at 1 mg/kg, iv measured during 2 mins to 24 hrs period post dose by LC/MS/MS method | 2015 | Bioorganic & medicinal chemistry, Jan-15, Volume: 23, Issue:2
| Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton's tyrosine kinase inhibitors. |
| AID671882 | Inhibition of anti-IgD antibody stimulated CD69 expression in mouse CIA model dosed prophylactically at 3 to 100 mg/kg, po measured 24 hrs post dose | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies. |
| AID1176491 | Apparent volume of distribution in Sprague-Dawley rat at 2 mg/kg, po measured during 2 mins to 24 hrs period post dose by LC/MS/MS method | 2015 | Bioorganic & medicinal chemistry, Jan-15, Volume: 23, Issue:2
| Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton's tyrosine kinase inhibitors. |
| AID1763485 | Antiinflammatory activity against collagen-induced arthritis Lewis rat model assessed as reduction in ankle swelling at 30 mg/kg/day, po administered from day 6 to 16 and measured on day 17 | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Discovery of potent and selective reversible Bruton's tyrosine kinase inhibitors. |
| AID1433171 | Clearance in Sprague-Dawley rat at 4 mg/kg, po by LC/MS/MS analysis | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
| Pyrrolo[2,3-b]pyridine derivatives as potent Bruton's tyrosine kinase inhibitors. |
| AID1176494 | Mean residence time (0 to t) in Sprague-Dawley rat at 1 mg/kg, iv measured during 2 mins to 24 hrs period post dose by LC/MS/MS method | 2015 | Bioorganic & medicinal chemistry, Jan-15, Volume: 23, Issue:2
| Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton's tyrosine kinase inhibitors. |
| AID1176487 | Cmax in Sprague-Dawley rat at 2 mg/kg, po measured during 2 mins to 24 hrs period post dose by LC/MS/MS method | 2015 | Bioorganic & medicinal chemistry, Jan-15, Volume: 23, Issue:2
| Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton's tyrosine kinase inhibitors. |
| AID1176481 | Inhibition of BTK (unknown origin) using biotin-labeled peptide substrate incubated for 1 hr by TR-FRET based HTRF kinase assay | 2015 | Bioorganic & medicinal chemistry, Jan-15, Volume: 23, Issue:2
| Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton's tyrosine kinase inhibitors. |
| AID1763456 | Inhibition of human ERG | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Discovery of potent and selective reversible Bruton's tyrosine kinase inhibitors. |
| AID1433168 | Cmax in Sprague-Dawley rat at 4 mg/kg, po by LC/MS/MS analysis | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
| Pyrrolo[2,3-b]pyridine derivatives as potent Bruton's tyrosine kinase inhibitors. |
| AID1433172 | Half life in Sprague-Dawley rat at 4 mg/kg, po by LC/MS/MS analysis | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
| Pyrrolo[2,3-b]pyridine derivatives as potent Bruton's tyrosine kinase inhibitors. |
| AID1176482 | Inhibition of BTK in human Ramos cells assessed as reduction in IgM-induced calcium influx incubated for 20 mins by Fluo-4 dye based fluorescence assay | 2015 | Bioorganic & medicinal chemistry, Jan-15, Volume: 23, Issue:2
| Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton's tyrosine kinase inhibitors. |
| AID1176497 | Half life in Sprague-Dawley rat at 2 mg/kg, po measured during 2 mins to 24 hrs period post dose by LC/MS/MS method | 2015 | Bioorganic & medicinal chemistry, Jan-15, Volume: 23, Issue:2
| Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton's tyrosine kinase inhibitors. |
| AID671879 | Competitive inhibition of BTK by TR-FRET based competitive assay | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies. |
| AID1176489 | AUC in Sprague-Dawley rat at 2 mg/kg, po measured during 2 mins to 24 hrs period post dose by LC/MS/MS method | 2015 | Bioorganic & medicinal chemistry, Jan-15, Volume: 23, Issue:2
| Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton's tyrosine kinase inhibitors. |
| AID1345824 | Human STE20 like kinase (SLK subfamily) | 2012 | The Journal of pharmacology and experimental therapeutics, Apr, Volume: 341, Issue:1
| RN486, a selective Bruton's tyrosine kinase inhibitor, abrogates immune hypersensitivity responses and arthritis in rodents. |
| AID1345617 | Human Bruton tyrosine kinase (Tec family) | 2012 | The Journal of pharmacology and experimental therapeutics, Apr, Volume: 341, Issue:1
| RN486, a selective Bruton's tyrosine kinase inhibitor, abrogates immune hypersensitivity responses and arthritis in rodents. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |