| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID594812 | Bioavailability in rat | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres. |
| AID604535 | Cmax in male rat at 20 mg/kg, po after 24 hrs | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID594804 | Inhibition of human MMP-13 | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres. |
| AID604607 | Antiangiogenic activity in cornea of mouse bFGF-induced corneal micropocket model assessed as inhibition of angiogenesis administered as BID | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID594805 | Inhibition of human MMP-14 | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres. |
| AID604449 | Inhibition of human MMP2 assessed as cleavage of fluorogenic peptide MCAPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorometric assay | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604455 | Inhibition of human MMP14 assessed as cleavage of fluorogenic peptide MCAPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorometric assay | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604529 | Selectivity ratio of IC50 for human MMP1 to IC50 for human MMP9 | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604623 | Oral bioavailability in female dog at 20 mg/kg after 24 hrs | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604541 | AUC (0 to infinity) in male dog at 20 mg/kg, po after 24 hrs | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604452 | Inhibition of human MMP8 assessed as cleavage of fluorogenic peptide MCAPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorometric assay | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604537 | Cmax in male mouse at 20 mg/kg, po after 24 hrs | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604460 | Cmax in rat at 20 mg/kg, po | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604463 | Oral bioavailability in rat at 20 mg/kg | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604617 | Cmax in female mouse at 20 mg/kg, po after 24 hrs | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604540 | AUC (0 to infinity) in male rat at 20 mg/kg, po after 24 hrs | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604471 | Cardioprotective activity in rat myocardial infarction model assessed inhibition of postinfection left ventricular dilation administered po qd for 4 weeks | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604534 | Tmax in cynomolgus monkey at 20 mg/kg, po after 24 hrs | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604448 | Inhibition of human MMP1 expressed in human HT-1080 cells assessed as cleavage of fluorogenic peptide MCAPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorometric assay | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID594803 | Inhibition of human MMP-9 | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres. |
| AID594809 | Cmax in rat | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres. |
| AID594802 | Inhibition of human MMP-8 | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres. |
| AID594800 | Inhibition of human MMP-3 | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres. |
| AID604622 | Oral bioavailability in female rat at 20 mg/kg after 24 hrs | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604451 | Inhibition of human MMP7 assessed as cleavage of fluorogenic peptide MCAPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorometric assay | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID594799 | Inhibition of human MMP-2 | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres. |
| AID604542 | AUC (0 to infinity) in cynomolgus monkey at 20 mg/kg, po after 24 hrs | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604538 | Cmax in cynomolgus monkey at 20 mg/kg, po after 24 hrs | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604533 | Tmax in male dog at 20 mg/kg, po after 24 hrs | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604543 | Oral bioavailability in male mouse at 20 mg/kg after 24 hrs | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604530 | Antiangiogenic activity in cornea of mouse bFGF-induced corneal micropocket model assessed as inhibition of angiogenesis at 5 mg/kg administered as BID | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604618 | AUC (0 to infinity) in female mouse at 20 mg/kg, po after 24 hrs | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604462 | Half life in rat at 20 mg/kg, po | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604461 | Plasma concentration in rat at 20 mg/kg, po | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604454 | Inhibition of human MMP13 assessed as cleavage of fluorogenic peptide MCAPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorometric assay | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID594801 | Inhibition of human MMP-7 | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres. |
| AID604614 | Tmax in female dog at 20 mg/kg, po after 24 hrs | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID594798 | Inhibition of human MMP-1 | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres. |
| AID604539 | AUC (0 to infinity) in male mouse at 20 mg/kg, po after 24 hrs | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604606 | Oral bioavailability in cynomolgus monkey at 20 mg/kg after 24 hrs | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604450 | Inhibition of human MMP3 assessed as cleavage of fluorogenic peptide MCAPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorometric assay | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604531 | Tmax in male mouse at 20 mg/kg, po after 24 hrs | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604616 | Cmax in female dog at 20 mg/kg, po after 24 hrs | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604464 | Antitumor activity against human PC3 cells xenografted in po dosed BALB/c nu/nu mouse assessed as tumor growth inhibition administered BID measured on 25 to 30 days | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604604 | Oral bioavailability in male rat at 20 mg/kg after 24 hrs | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604615 | Cmax in female rat at 20 mg/kg, po after 24 hrs | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604620 | AUC (0 to infinity) in female dog at 20 mg/kg, po after 24 hrs | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604528 | Selectivity ratio of IC50 for human MMP1 to IC50 for human MMP2 | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604532 | Tmax in male rat at 20 mg/kg, po after 24 hrs | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604619 | AUC (0 to infinity) in female rat at 20 mg/kg, po after 24 hrs | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604621 | Oral bioavailability in female mouse at 20 mg/kg after 24 hrs | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604612 | Tmax in female mouse at 20 mg/kg, po after 24 hrs | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604526 | Cardioprotective activity in rat myocardial infarction model assessed inhibition of left ventricular dilation at 10 mg/kg, po qd for 4 weeks (Rvb = 0.59 +/- 0.02 mL) | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604453 | Inhibition of human MMP9 assessed as cleavage of fluorogenic peptide MCAPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorometric assay | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604527 | Selectivity ratio of IC50 for human MMP13 to IC50 for human MMP1 | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID594808 | Half life in rat | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres. |
| AID604605 | Oral bioavailability in male dog at 20 mg/kg after 24 hrs | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604536 | Cmax in male dog at 20 mg/kg, po after 24 hrs | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| AID604613 | Tmax in female rat at 20 mg/kg, po after 24 hrs | 2010 | Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
| Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |