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. |
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. |
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. |
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. |
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. |
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. |
AID1628666 | Selectivity index, ratio of IC50 for inhibition of N-terminal polyHis tagged full length recombinant PI3Kgamma (114 to 1102 residues) (unknown origin) expressed in Hi5 cells co-expressing p85 o IC50 for polyHis tagged full length recombinant PI3Kdelta (un | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
| Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)eth |
AID1628665 | Selectivity index, ratio of IC50 for inhibition of polyHis tagged full length recombinant PI3Kbeta (unknown origin) expressed in Sf9 cells co-expressing p85 to IC50 for polyHis tagged full length recombinant PI3Kdelta (unknown origin) expressed in Sf9 cel | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
| Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)eth |
AID1628672 | Oral bioavailability in Sprague-Dawley rat at 2 mg/kg by by LC-MS method | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
| Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)eth |
AID1628650 | Inhibition of polyHis tagged full length recombinant PI3Kdelta (unknown origin) expressed in Sf9 cells co-expressing p85 incubated for 20 mins by alpha screen assay | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
| Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)eth |
AID1628653 | Inhibition of N-terminal polyHis tagged full length recombinant PI3Kgamma (114 to 1102 residues) (unknown origin) expressed in Hi5 cells co-expressing p85 incubated for 20 mins by alpha screen assay | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
| Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)eth |
AID1628671 | Fraction unbound in rat plasma at 5 uM by LC/MS assay based ultracentrifugation method | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
| Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)eth |
AID1628659 | Inhibition of CYP2D6 (unknown origin) at 3 uM using midazolam substrate by LC-MS method | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
| Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)eth |
AID1628667 | Inhibition of PI3Kdelta in human whole blood assessed as inhibition of Anti-IgD antibody-induced AKT Ser473 phosphorylation pre-incubated for 60 mins before Anti-IgD antibody stimulation | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
| Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)eth |
AID1628655 | Inhibition of PI3Kdelta in BALB/c mouse B cells assessed as reduction in Anti-IgM induced AKT Ser473 phosphorylation pre-incubated for 45 mins before Anti-IgM stimulation | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
| Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)eth |
AID1628654 | Inhibition of cell proliferation of human B cells pre-incubated for 30 mins before anti-IgM/CD40L stimulation and measured after 72 hrs by [3H]thymidine incorporation assay | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
| Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)eth |
AID1628657 | Clearance in human liver microsomes assessed as drug turnover level at 1 uM incubated for 30 mins in presence of NADPH | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
| Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)eth |
AID1628651 | Inhibition of polyHis tagged full length recombinant PI3Kalpha (unknown origin) expressed in Sf9 cells co-expressing p85 incubated for 20 mins by alpha screen assay | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
| Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)eth |
AID1628660 | Activation of human PXR assessed as remaining activity at 2 uM relative to untreated control | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
| Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)eth |
AID1628662 | Clearance in Sprague-Dawley rat at 0.5 mg/kg, iv by by LC-MS method | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
| Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)eth |
AID1628670 | Fraction unbound in human plasma at 5 uM by LC/MS assay based ultracentrifugation method | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
| Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)eth |
AID1628661 | Activation of human PXR assessed as remaining activity at 10 uM relative to untreated control | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
| Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)eth |
AID1628663 | Unbound clearance in Sprague-Dawley rat at 0.5 mg/kg, iv by by LC-MS method | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
| Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)eth |
AID1628664 | Selectivity index, ratio of IC50 for inhibition of polyHis tagged full length recombinant PI3Kalpha (unknown origin) expressed in Sf9 cells co-expressing p85 to IC50 for polyHis tagged full length recombinant PI3Kdelta (unknown origin) expressed in Sf9 ce | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
| Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)eth |
AID1628669 | Apparent permeability in LLC-PK1 cells by LC-MS method | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
| Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)eth |
AID1628668 | Aqueous equilibrium solubility at room temperature after 72 hrs at pH 7.4 by HPLC | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
| Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)eth |
AID1628652 | Inhibition of polyHis tagged full length recombinant PI3Kbeta (unknown origin) expressed in Sf9 cells co-expressing p85 incubated for 20 mins by alpha screen assay | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
| Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)eth |
AID1628658 | Inhibition of CYP3A4 (unknown origin) at 3 uM using midazolam substrate by LC-MS method | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
| Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)eth |
AID1628656 | Clearance in rat liver microsomes assessed as drug turnover level at 1 uM incubated for 30 mins in presence of NADPH | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
| Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)eth |
AID1345786 | Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma (Phosphatidylinositol kinases) | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and in vivo evaluation of (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease. |
AID1345748 | Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta (Phosphatidylinositol kinases) | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and in vivo evaluation of (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease. |
AID1345749 | Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha (Phosphatidylinositol kinases) | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and in vivo evaluation of (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease. |
AID1345778 | Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta (Phosphatidylinositol kinases) | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and in vivo evaluation of (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease. |
AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Discovery and in vivo evaluation of (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |